S. Wittlin

发表

Cell Penetration, Herbicidal Activity, and in-vivo-Toxicity of Oligo-Arginine Derivatives and of Novel Guanidinium-Rich Compounds Derived from the Biopolymer Cyanophycin.

D. Hilvert, M. Ebert, D. Seebach, 2018, Helvetica chimica acta.

Antiprotozoal Selectivity of Diimidazoline N-Phenylbenzamides.

M. Kaiser, Yuxiang Dong, Xiaofang Wang, 2015, ACS infectious diseases.

Two successful decades of Swiss collaborations to develop new anti-malarials

M. Tanner, R. Hooft van Huijsduijnen, T. Wells, 2019, Malaria Journal.

Synthesis, structure-activity relationship, and mode-of-action studies of antimalarial reversed chloroquine compounds.

R. Brun, S. Burgess, S. Wittlin, 2010, Journal of medicinal chemistry.

Okundoperoxide, a bicyclic cyclofarnesylsesquiterpene endoperoxide from Scleria striatinux with antiplasmodial activity.

T. Hoye, S. Efange, R. Brun, 2009, Journal of natural products.

Anti-malarial Activity in the Mouse Model Dihydroorotate Dehydrogenase with Plasmodium falciparum Novel Inhibitors of Molecular Bases of Disease :

Margaret A. Phillips, Elizabeth J. Goldsmith, Dyann F. Wirth, 2010 .

A novel multiple-stage antimalarial agent that inhibits protein synthesis

David W. Gray, E. Winzeler, S. Meister, 2015, Nature.

In Vitro and In Vivo Activity of Solithromycin (CEM-101) against Plasmodium Species

D. Fidock, J. Lotharius, E. Ekland, 2011, Antimicrobial Agents and Chemotherapy.

Synthesis and in vitro antiprotozoal activities of 5-phenyliminobenzo[a]phenoxazine derivatives.

J. Ge, R. Brun, M. Ihara, 2011, Bioorganic & medicinal chemistry letters.

Discovery of Novel Benzo[a]phenoxazine SSJ-183 as a Drug Candidate for Malaria.

J. Ge, S. Charman, R. Brun, 2010, ACS medicinal chemistry letters.

SYNTHESIS AND BIOLOGICAL PROPERTIES OF A RHODACYANINE DERIVATIVE, SSJ-127, HAVING HIGH EFFICACY AGAINST MALARIA PROTOZOA

R. Brun, M. Ihara, K. Pudhom, 2009 .

Malaria-infected mice are cured by oral administration of new artemisinin derivatives.

T. Shapiro, J. Chollet, R. Brun, 2008, Journal of medicinal chemistry.

Global metabolic responses of NMRI mice to an experimental Plasmodium berghei infection.

M. Tanner, J. Utzinger, B. Singer, 2008, Journal of proteome research.

Structure-activity relationship studies of orally active antimalarial 3,5-substituted 2-aminopyridines.

K. Chibale, M. Witty, S. Charman, 2012, Journal of Medicinal Chemistry.

Antimalarial pantothenamide metabolites target acetyl-CoA synthesis in Plasmodium falciparum

M. Llinás, P. Jansen, K. Dechering, 2018, bioRxiv.

AntigenCyRPA as Candidate Malaria Vaccine -Infected Mice Designates the falciparum Plasmodium Passive Immunoprotection of

G. Pluschke, H. Matile, T. Voss, 2012 .

Benzo[b]quinolizinium Derivatives Have a Strong Antimalarial Activity and Inhibit Indoleamine Dioxygenase

S. Rahlfs, K. Becker, H. Ihmels, 2015, Antimicrobial Agents and Chemotherapy.

Weak base dispiro-1,2,4-trioxolanes: potent antimalarial ozonides.

J. Karle, J. Chollet, S. Charman, 2007, Bioorganic & medicinal chemistry letters.

First-in-man safety and pharmacokinetics of synthetic ozonide OZ439 demonstrates an improved exposure profile relative to other peroxide antimalarials

C. Siethoff, S. Charman, S. Duparc, 2012, British journal of clinical pharmacology.

In vitro activity of anti-malarial ozonides against an artemisinin-resistant isolate

Brice Campo, P. Mäser, S. Wittlin, 2017, Malaria Journal.

Structure-Activity Relationship of the Antimalarial Ozonide Artefenomel (OZ439).

David M. Shackleford, J. Chollet, S. Charman, 2017, Journal of medicinal chemistry.

In vitro and in vivo characterization of the antimalarial lead compound SSJ-183 in Plasmodium models

David M. Shackleford, S. Charman, R. Brun, 2013, Drug design, development and therapy.

3-Alkoxy-1,2-Dioxolanes: Synthesis and Evaluation as Potential Antimalarial Agents.

S. Wittlin, P. Dussault, Charles E. Schiaffo, 2011, ACS medicinal chemistry letters.

The structure and antimalarial activity of dispiro-1,2,4,5-tetraoxanes derived from (+)-dihydrocarvone.

J. Chollet, Yuxiang Dong, J. Vennerstrom, 2010, Bioorganic & medicinal chemistry letters.

Synthesis and in vitro antimalarial activity of spiro-analogues of peroxyplakoric acids

Qi Zhang, S. Wittlin, Yikang Wu, 2009 .

Spiroadamantyl 1,2,4-trioxolane, 1,2,4-trioxane, and 1,2,4-trioxepane pairs: relationship between peroxide bond iron(II) reactivity, heme alkylation efficiency, and antimalarial activity.

J. K. Wood, J. Chollet, S. Charman, 2009, Bioorganic & medicinal chemistry letters.

Structure-Activity Relationship Studies of Orally Active Antimalarial 2,4-Diamino-thienopyrimidines.

K. Chibale, Dale Taylor, M. Witty, 2015, Journal of medicinal chemistry.

Identification of Taxreb107 as a lactogenic hormone responsive gene in mammary epithelial cells.

J. Visvader, G. Lindeman, K. Sutherland, 2003, Biochimica et biophysica acta.

Discovery and Structure-Activity Relationships of Quinazolinone-2-carboxamide Derivatives as Novel Orally Efficacious Antimalarials.

David M. Shackleford, Laura M Sanz, K. Dechering, 2021, Journal of medicinal chemistry.

Repositioning and Characterization of 1-(Pyridin-4-yl)pyrrolidin-2-one Derivatives as Plasmodium Cytoplasmic Prolyl-tRNA Synthetase Inhibitors

David M. Shackleford, D. Fidock, Laura M Sanz, 2021, ACS infectious diseases.

Ensemble modeling highlights importance of understanding parasite-host behavior in preclinical antimalarial drug development

M. Penny, J. Möhrle, J. Dingemanse, 2020, Scientific Reports.

Identification of a Potential Antimalarial Drug Candidate from a Series of 2-Aminopyrazines by Optimization of Aqueous Solubility and Potency across the Parasite Life Cycle.

E. Winzeler, S. Meister, K. Chibale, 2016, Journal of medicinal chemistry.

A Novel Pyrazolopyridine with in Vivo Activity in Plasmodium berghei- and Plasmodium falciparum-Infected Mouse Models from Structure-Activity Relationship Studies around the Core of Recently Identified Antimalarial Imidazopyridazines.

E. Winzeler, S. Meister, K. Chibale, 2015, Journal of medicinal chemistry.

Medicinal chemistry optimization of antiplasmodial imidazopyridazine hits from high throughput screening of a SoftFocus kinase library: part 1.

K. Chibale, Dale Taylor, M. Witty, 2014, Journal of medicinal chemistry.

Spiro- and dispiro-1,2-dioxolanes: contribution of iron(II)-mediated one-electron vs two-electron reduction to the activity of antimalarial peroxides.

J. Chollet, S. Charman, D. Creek, 2007, Journal of medicinal chemistry.

Identification of a 1,2,4,5-tetraoxane antimalarial drug-development candidate (RKA 182) with superior properties to the semisynthetic artemisinins.

B. K. Park, V. Barton, G. Nixon, 2010, Angewandte Chemie.

Antimalarial Mannoxanes: Hybrid Antimalarial Drugs with Outstanding Oral Activity Profiles and A Potential Dual Mechanism of Action

S. Parapini, D. Taramelli, R. Amewu, 2011, ChemMedChem.

Discovery of dual function acridones as a new antimalarial chemotype

A. Janowsky, Robert A. Johnson, R. Brun, 2009, Nature.

A fast-killing tyrosine amide ((S)-SW228703) with blood and liver-stage antimalarial activity associated with the Cyclic Amine Resistance Locus (PfCARL)

E. Winzeler, M. Phillips, F. Gamo, 2022, bioRxiv.

Novel Antimalarial Tetrazoles and Amides Active against the Hemoglobin Degradation Pathway in Plasmodium falciparum.

E. Winzeler, D. Fidock, M. Phillips, 2021, Journal of medicinal chemistry.

Reaction hijacking of tyrosine tRNA synthetase as a whole-of-life-cycle antimalarial strategy

E. Winzeler, M. Parker, C. Morton, 2022, Science.

Discovery and Characterization of Potent, Efficacious, Orally Available Antimalarial Plasmepsin X Inhibitors and Preclinical Safety Assessment of UCB7362

Richard D. Taylor, D. Goldberg, A. Cowman, 2022, Journal of medicinal chemistry.

A small-molecule myosin inhibitor as a targeted multi-stage antimalarial

Paul V. Ruijgrok, E. Winzeler, J. Spudich, 2022, bioRxiv.

Mechanisms and kinetics of procathepsin D activation.

D. Stover, F. Hofmann, S. Wittlin, 1999, European journal of biochemistry.

Potent antimalarial 1,2,4-trioxanes through perhydrolysis of epoxides.

S. Wittlin, Yikang Wu, Hong-Dong Hao, 2013, Chemistry.

Simple analogues of qinghaosu (artemisinin).

Yun Li, S. Wittlin, Yikang Wu, 2012, Chemistry, an Asian journal.

Antimalarial Spiro-Bridged 1,2-Dioxolanes via Intramolecular Addition of Peroxycarbenium Ions to C-C Double Bonds

S. Wittlin, Yikang Wu, Yun Li, 2012 .

ACCESS TO SOME UV CHROMOPHORE-CONTAINING ANTIMALARIAL TRIOXANES USING HYDROGEN PEROXIDE AS SOURCE OF THE PEROXY BONDS

S. Wittlin, Yikang Wu, Yun Li, 2012 .

Spiro and dispiro-1,2,4-trioxolanes as antimalarial peroxides: charting a workable structure-activity relationship using simple prototypes.

J. Karle, J. Chollet, S. Charman, 2005, Journal of medicinal chemistry.

Soudanones A-G: Antifungal Isochromanones from the Ascomycetous Fungus Cadophora sp. Isolated from an Iron Mine.

R. Blanchette, B. Held, C. Salomon, 2015, Journal of natural products.

Identification of steroid-like natural products as antiplasmodial agents by 2D and 3D similarity-based virtual screening.

K. Chibale, S. Wittlin, Gurminder Kaur, 2017, MedChemComm.

Occurrence of Sesquiterpene Derivatives in Scleria Striatonux De Wild (Cyperaceae)

K. Hostettmann, S. Efange, R. Brun, 2009, Natural product communications.

Plasmodium berghei ANKA: Selection of resistance to piperaquine and lumefantrine in a mouse model

A. Nzila, A. Bell, J. Chollet, 2009, Experimental parasitology.

Inhibitors of plasmodial serine hydroxymethyltransferase (SHMT): cocrystal structures of pyrazolopyrans with potent blood- and liver-stage activities.

F. Diederich, T. Mietzner, C. Pinthong, 2015, Journal of medicinal chemistry.

Synthesis of cyanine dyes and investigation of their in vitro antiprotozoal activities

J. Ge, R. Brun, M. Ihara, 2012 .

The structure-activity relationship of the antimalarial ozonide arterolane (OZ277).

J. Chollet, S. Charman, W. Charman, 2010, Journal of medicinal chemistry.

Identification of Fast-Acting 2,6-Disubstituted Imidazopyridines That Are Efficacious in the in Vivo Humanized Plasmodium falciparum NODscidIL2Rγ null Mouse Model of Malaria.

K. Chibale, Dale Taylor, K. Wicht, 2018, Journal of medicinal chemistry.

Structure-activity-relationship studies around the 2-amino group and pyridine core of antimalarial 3,5-diarylaminopyridines lead to a novel series of pyrazine analogues with oral in vivo activity.

K. Chibale, M. Witty, S. Charman, 2013, Journal of medicinal chemistry.

3,5-Diaryl-2-aminopyridines as a novel class of orally active antimalarials demonstrating single dose cure in mice and clinical candidate potential.

David M. Shackleford, K. Chibale, M. Witty, 2012, Journal of medicinal chemistry.

Metabolic, Pharmacokinetic, and Activity Profile of the Liver Stage Antimalarial (RC-12)

D. Kyle, S. Charman, C. Kocken, 2022, ACS omega.

Novel in vivo active anti-malarials based on a hydroxy-ethyl-amine scaffold.

R. de Kanter, S. Wittlin, C. Boss, 2013, Bioorganic & medicinal chemistry letters.

Antimalarial activity of novel pyrrolizidinyl derivatives of 4-aminoquinoline.

Silvia Parapini, Nicoletta Basilico, Donatella Taramelli, 2008, Bioorganic & medicinal chemistry letters.

Comparative antimalarial activities and ADME profiles of ozonides (1,2,4-trioxolanes) OZ277, OZ439, and their 1,2-dioxolane, 1,2,4-trioxane, and 1,2,4,5-tetraoxane isosteres.

J. Chollet, S. Charman, E. Ryan, 2013, Journal of medicinal chemistry.

Lysyl-tRNA synthetase as a drug target in malaria and cryptosporidiosis

Juan A. Bueren-Calabuig, Andrei V. Pisliakov, David W. Gray, 2019, Proceedings of the National Academy of Sciences.

Discovery of a Quinoline-4-carboxamide Derivative with a Novel Mechanism of Action, Multistage Antimalarial Activity, and Potent in Vivo Efficacy

David W. Gray, E. Winzeler, S. Meister, 2016, Journal of medicinal chemistry.

2,4-Diaminothienopyrimidines as orally active antimalarial agents.

K. Chibale, Dale Taylor, M. Witty, 2014, Journal of medicinal chemistry.

Trisubstituted Pyrimidines as Efficacious and Fast-Acting Antimalarials

E. Winzeler, S. Meister, S. Norval, 2016, Journal of medicinal chemistry.

Novel orally active antimalarial thiazoles.

K. Chibale, M. Witty, S. Charman, 2011, Journal of medicinal chemistry.

Thiazolopyrimidine Inhibitors of 2‐Methylerythritol 2,4‐Cyclodiphosphate Synthase (IspF) from Mycobacterium tuberculosis and Plasmodium falciparum

F. Diederich, W. Eisenreich, A. Bacher, 2010, ChemMedChem.

Synthesis and in vitro antiprotozoal activities of water-soluble, inexpensive phenothiazinium chlorides

Jian‐mei Lu, J. Ge, R. Brun, 2011 .

Bioisosteric ferrocenyl aminoquinoline-benzimidazole hybrids: Antimicrobial evaluation and mechanistic insights.

K. Chibale, D. Warner, Gregory S. Smith, 2019, European journal of medicinal chemistry.

In vitro antiplasmodial activity and toxicity assessment of some plants from Nigerian ethnomedicine

A. Sowunmi, R. Brun, M. Falade, 2011, Pharmaceutical biology.

Ancient Chinese Methods Are Remarkably Effective for the Preparation of Artemisinin-Rich Extracts of Qing Hao with Potent Antimalarial Activity

P. Linley, R. Brun, S. Wittlin, 2010, Molecules.

Isothermal Microcalorimetry, a New Tool to Monitor Drug Action against Trypanosoma brucei and Plasmodium falciparum

A. Steinhuber, R. Brun, A. Trampuz, 2012, PLoS neglected tropical diseases.

Identification of an antimalarial synthetic trioxolane drug development candidate

Christian Scheurer, Jonathan L. Vennerstrom, Susan A. Charman, 2004, Nature.

Structure-activity relationships for ferriprotoporphyrin IX association and β-hematin inhibition by 4-aminoquinolines using experimental and ab initio methods.

K. Chibale, T. Egan, D. Kuter, 2013, Bioorganic & medicinal chemistry.

UCT943, a Next-Generation Plasmodium falciparum PI4K Inhibitor Preclinical Candidate for the Treatment of Malaria

R. Price, K. Chibale, Dale Taylor, 2018, Antimicrobial Agents and Chemotherapy.

Antiparasitic agents: new drugs on the horizon.

P. Mäser, R. Brun, M. Kaiser, 2012, Current opinion in pharmacology.

From Magic Bullet to Magic Bomb: Reductive Bioactivation of Antiparasitic Agents.

P. Mäser, S. Wittlin, 2021, ACS infectious diseases.

Synthesis and biological characterisation of ester and amide derivatives of fusidic acid as antiplasmodial agents.

K. Chibale, Peter J. Smith, John Okombo, 2017, Bioorganic & medicinal chemistry letters.

Arylmethylamino steroids as antiparasitic agents

S. Rahlfs, K. Becker, E. Davioud‐Charvet, 2017, Nature Communications.

Incorporation of an intramolecular hydrogen bonding motif in the side chain of antimalarial benzimidazoles.

K. Chibale, S. Wittlin, Henrietta D Attram, 2019, MedChemComm.

Tetracaine, propranolol and trifluoperazine inhibit thyrotropin releasing hormone-induced prolactin secretion from GH3 cells by displacing membrane calcium: further evidence that TRH acts to mobilize cellular calcium.

M. Gershengorn, S. Wittlin, C. Thaw, 1982, Endocrinology.

Structure-Activity Relationship Studies and Plasmodium Life Cycle Profiling Identifies Pan-Active N-Aryl-3-trifluoromethyl Pyrido[1,2- a]benzimidazoles Which Are Efficacious in an in Vivo Mouse Model of Malaria.

K. Chibale, T. Egan, John Okombo, 2019, Journal of medicinal chemistry.

, 2 ‐ a ] benzimidazoles Which Are E ffi cacious in an in Vivo Mouse Model of Malaria

K. Chibale, T. Egan, John Okombo, 2019 .

Antimalarial Pyrido[1,2-a]benzimidazoles: Lead Optimization, Parasite Life Cycle Stage Profile, Mechanistic Evaluation, Killing Kinetics, and in Vivo Oral Efficacy in a Mouse Model.

K. Chibale, T. Egan, John Okombo, 2017, Journal of medicinal chemistry.

Passive Immunoprotection of Plasmodium falciparum-Infected Mice Designates the CyRPA as Candidate Malaria Vaccine Antigen

G. Pluschke, H. Matile, T. Voss, 2012, The Journal of Immunology.

CPAP is a novel stat5-interacting cofactor that augments stat5-mediated transcriptional activity.

Monilola A. Olayioye, J. Visvader, E. Sum, 2002, Molecular endocrinology.

The Activities of Current Antimalarial Drugs on the Life Cycle Stages of Plasmodium: A Comparative Study with Human and Rodent Parasites

E. Winzeler, S. Meister, D. Plouffe, 2012, PLoS medicine.

Peroxide Bond-Dependent Antiplasmodial Specificity of Artemisinin and OZ277 (RBx11160)

R. Brun, H. Matile, M. Kaiser, 2007, Antimicrobial Agents and Chemotherapy.

A long-duration dihydroorotate dehydrogenase inhibitor (DSM265) for prevention and treatment of malaria

Farah El Mazouni, T. Laird, P. Rathod, 2015, Science Translational Medicine.

Antimalarial N 1,N 3-Dialkyldioxonaphthoimidazoliums: Synthesis, Biological Activity, and Structure-activity Relationships.

K. Tan, L. Birkholtz, S. Wittlin, 2019, ACS medicinal chemistry letters.

Antimalarial pantothenamide metabolites target acetyl–coenzyme A biosynthesis in Plasmodium falciparum

M. Llinás, P. Jansen, K. Dechering, 2019, Science Translational Medicine.

Fast in vitro methods to determine the speed of action and the stage-specificity of anti-malarials in Plasmodium falciparum

K. Chibale, Xavier C Ding, D. Leroy, 2013, Malaria Journal.

Cysteine-Rich Protective Antigen (CyRPA) as promising blood-stage candidate protein for inclusion in a malaria subunit vaccine

G. Pluschke, H. Matile, S. Wittlin, 2012, Malaria Journal.

Comparative embryotoxicity of different antimalarial peroxides: in vitro study using the rat whole embryo culture model (WEC).

P. Colombo, M. Longo, J. Craft, 2010, Reproductive toxicology.

Synthetic ozonide drug candidate OZ439 offers new hope for a single-dose cure of uncomplicated malaria

Christian Scheurer, Lukas Stingelin, David M. Shackleford, 2011, Proceedings of the National Academy of Sciences.

The bacterial redox signaller pyocyanin as an antiplasmodial agent: comparisons with its thioanalog methylene blue

K. Fritz-Wolf, S. Rahlfs, R. Schirmer, 2011, Redox report : communications in free radical research.

New Amidated 3,6-Diphenylated Imidazopyridazines with Potent Antiplasmodium Activity Are Dual Inhibitors of Plasmodium Phosphatidylinositol-4-kinase and cGMP-Dependent Protein Kinase.

S. Fienberg, K. Chibale, Dale Taylor, 2020, ACS infectious diseases.

Triclosan is minimally effective in rodent malaria models

A. Fairlamb, S. Croft, D. Fidock, 2011, Nature Medicine.

The catalytic subunit of Plasmodium falciparum casein kinase 2 is essential for gametocytogenesis

H. Beck, Nicolas M. B. Brancucci, T. Voss, 2021, Communications biology.

Antimalarial efficacy of MMV390048, an inhibitor of Plasmodium phosphatidylinositol 4-kinase

David M. Shackleford, G. Drewes, M. Bantscheff, 2017, Science Translational Medicine.

Aminoindoles, a Novel Scaffold with Potent Activity against Plasmodium falciparum

Bradley I. Coleman, R. Barker, D. Wirth, 2011, Antimicrobial Agents and Chemotherapy.

The antimalarial MMV688533 provides potential for single-dose cures with a high barrier to Plasmodium falciparum parasite resistance

R. Price, P. Rosenthal, D. Fidock, 2021, Science Translational Medicine.

7-N-Substituted-3-oxadiazole Quinolones with Potent Antimalarial Activity Target the Cytochrome bc1 Complex

E. Winzeler, A. Cowman, G. V. van Dooren, 2023, ACS infectious diseases.

Anti-malarial ozonides OZ439 and OZ609 tested at clinically relevant compound exposure parameters in a novel ring-stage survival assay

P. Mäser, D. Leroy, S. Wittlin, 2019, Malaria Journal.

Differential hypermethylation of SOCS genes in ovarian and breast carcinomas

Sergio Wittlin, J. Visvader, I. Campbell, 2004, Oncogene.

SOCS1 deficiency results in accelerated mammary gland development and rescues lactation in prolactin receptor-deficient mice.

J. G. Zhang, J. Visvader, W. Alexander, 2001, Genes & development.

Two promoters within the human LMO4 gene contribute to its overexpression in breast cancer cells.

Sergio Wittlin, J. Visvader, E. Sum, 2003, Genomics.

Socs2 and elf5 mediate prolactin-induced mammary gland development.

J. Visvader, W. Alexander, K. Blazek, 2006, Molecular endocrinology.

The 3-phosphoinositide–dependent protein kinase 1 is an essential upstream activator of protein kinase A in malaria parasites

P. Mäser, I. Vakonakis, Nicolas M. B. Brancucci, 2021, PLoS biology.

The catalytic subunit of Plasmodium falciparum casein kinase 2 is essential for gametocytogenesis

H. Beck, Nicolas M. B. Brancucci, T. Voss, 2021, Communications Biology.

Medicinal chemistry optimization of antiplasmodial imidazopyridazine hits from high throughput screening of a softfocus kinase library: part 2.

K. Chibale, Dale Taylor, M. Witty, 2014, Journal of medicinal chemistry.

Comparative Ex Vivo Activity of Novel Endoperoxides in Multidrug-Resistant Plasmodium falciparum and P. vivax

R. Price, E. Kenangalem, N. Anstey, 2012, Antimicrobial Agents and Chemotherapy.

Plasmodium falciparum and P . vivax Endoperoxides in Multidrug-Resistant Activity of Novel Ex Vivo Comparative

Frans, Piera, R. Price, 2012 .

Antimalarial Lead-Optimization Studies on a 2,6-Imidazopyridine Series within a Constrained Chemical Space To Circumvent Atypical Dose-Response Curves against Multidrug Resistant Parasite Strains.

C. Eyermann, K. Chibale, Dale Taylor, 2018, Journal of medicinal chemistry.

Identification of 2,4-Disubstituted Imidazopyridines as Hemozoin Formation Inhibitors with Fast-Killing Kinetics and In Vivo Efficacy in the Plasmodium falciparum NSG Mouse Model.

K. Chibale, T. Egan, Dale Taylor, 2020, Journal of medicinal chemistry.

Novel 3-Trifluoromethyl-1,2,4-oxadiazole Analogues of Astemizole with Multi-stage Antiplasmodium Activity and In Vivo Efficacy in a Plasmodium berghei Mouse Malaria Infection Model.

K. Chibale, T. Egan, Dale Taylor, 2022, Journal of medicinal chemistry.

Comparison of SYBR Green I-, PicoGreen-, and [3H]-hypoxanthine-based assays for in vitro antimalarial screening of plants from Nigerian ethnomedicine

C. Happi, A. Sowunmi, R. Brun, 2010, Parasitology Research.

Prodrugs of reverse fosmidomycin analogues.

A. Bacher, B. Mordmüller, T. Kurz, 2015, Journal of medicinal chemistry.

Ensemble modeling highlights importance of understanding parasite-host behavior in preclinical antimalarial drug development

M. Penny, J. Möhrle, J. Dingemanse, 2020, Scientific Reports.

Discovery of FNDR-20123, a histone deacetylase inhibitor for the treatment of Plasmodium falciparum malaria

S. Narayanan, R. Shandil, S. Wittlin, 2020, Malaria Journal.

Preclinical Evaluation of the Antifolate QN254, 5-Chloro- N′6′-(2,5-Dimethoxy-Benzyl)-Quinazoline-2,4,6-Triamine, as an Antimalarial Drug Candidate

A. Nzila, Y. Yuthavong, N. Ma, 2010, Antimicrobial Agents and Chemotherapy.

Plasmodium vivax: in vitro susceptibility of blood stages to synthetic trioxolane compounds and the diamidine DB75.

A. Thomas, R. Brun, C. Kocken, 2006, Experimental parasitology.

CRISPR‐Cas9‐modified pfmdr1 protects Plasmodium falciparum asexual blood stages and gametocytes against a class of piperazine‐containing compounds but potentiates artemisinin‐based combination therapy partner drugs

Victoria C. Corey, E. Winzeler, D. Fidock, 2016, Molecular microbiology.

Open Source Drug Discovery: Highly Potent Antimalarial Compounds Derived from the Tres Cantos Arylpyrroles

Julie Clark, George Papadatos, Jeremy N. Burrows, 2016, ACS central science.

Synthesis of fusidic acid bioisosteres as antiplasmodial agents and molecular docking studies in the binding site of elongation factor-G

K. Chibale, Peter J. Smith, S. Wittlin, 2015 .

Identification and Deconvolution of Cross-Resistance Signals from Antimalarial Compounds Using Multidrug-Resistant Plasmodium falciparum Strains

E. Bilsland, T. Egan, D. V. van Schalkwyk, 2014, Antimicrobial Agents and Chemotherapy.

UV-triggered Affinity Capture Identifies Interactions between the Plasmodium falciparum Multidrug Resistance Protein 1 (PfMDR1) and Antimalarial Agents in Live Parasitized Cells*

P. Roepe, D. Fidock, M. Akabas, 2013, The Journal of Biological Chemistry.

Identification of a new chemical class of antimalarials.

Zbynek Bozdech, R. Brun, M. Kaiser, 2012, The Journal of infectious diseases.

Screening medicinal plants for the detection of novel antimalarial products applying the inhibition of β-hematin formation.

K. Hostettmann, S. Wittlin, J. Ioset, 2011, Journal of pharmaceutical and biomedical analysis.

Optimization of Potent Inhibitors of P. falciparum Dihydroorotate Dehydrogenase for the Treatment of Malaria.

R. Barker, B. Muñoz, J. Cortese, 2011, ACS medicinal chemistry letters.

Antimalarial Benzimidazole Derivatives Incorporating Phenolic Mannich Base Side Chains Inhibit Microtubule and Hemozoin Formation: Structure-Activity Relationship and In Vivo Oral Efficacy Studies.

K. Chibale, G. Dziwornu, L. Birkholtz, 2021, Journal of medicinal chemistry.

3-Hydroxy-propanamidines, a New Class of Orally Active Antimalarials Targeting Plasmodium falciparum.

D. Fidock, B. Mordmüller, John Okombo, 2021, Journal of medicinal chemistry.

Multistage Antiplasmodium Activity of Astemizole Analogues and Inhibition of Hemozoin Formation as a Contributor to Their Mode of Action.

K. Chibale, T. Egan, Dale Taylor, 2018, ACS infectious diseases.

Erratum: Antimalarial pantothenamide metabolites target acetyl-coenzyme A biosynthesis in Plasmodium falciparum (Science Translational Medicine DOI: 10.1126/scitranslmed.aas9917)

M. Llinás, P. Jansen, K. Dechering, 2021 .

Methotrexate and aminopterin lack in vivo antimalarial activity against murine malaria species.

A. Nzila, S. Wittlin, D. Kiboi, 2009, Experimental parasitology.

Discovery and Characterization of ACT‐451840: an Antimalarial Drug with a Novel Mechanism of Action

R. Brun, S. Delahaye, S. Wittlin, 2016, ChemMedChem.

Discovery of FNDR-20123, a histone deacetylase inhibitor for the treatment of Plasmodium falciparum malaria

S. Narayanan, R. Shandil, S. Wittlin, 2020, Malaria journal.

Comparative Antimalarial Activities of Six Pairs of 1,2,4,5-Tetraoxanes (Peroxide Dimers) and 1,2,4,5,7,8-Hexaoxonanes (Peroxide Trimers)

J. K. Wood, James K. Wood, J. Chollet, 2007, Antimicrobial Agents and Chemotherapy.

Histone Methyltransferase Inhibitors Are Orally Bioavailable, Fast-Acting Molecules with Activity against Different Species Causing Malaria in Humans

N. A. Malmquist, R. Sinden, F. Gamo, 2014, Antimicrobial Agents and Chemotherapy.

Preclinical characterization and target validation of the antimalarial pantothenamide MMV693183

P. Rosenthal, M. Llinás, D. Fidock, 2021, bioRxiv.

Design of proteasome inhibitors with oral efficacy in vivo against Plasmodium falciparum and selectivity over the human proteasome

E. Winzeler, L. Tilley, D. Fidock, 2021, Proceedings of the National Academy of Sciences.

Investigating Sulfoxide-to-Sulfone Conversion as a Prodrug Strategy for a Phosphatidylinositol 4-Kinase Inhibitor in a Humanized Mouse Model of Malaria

K. Chibale, Dale Taylor, G. Basarab, 2018, Antimicrobial Agents and Chemotherapy.

Long-Lasting and Fast-Acting in Vivo Efficacious Antiplasmodial Azepanylcarbazole Amino Alcohol.

P. Hewitt, D. Picard, S. Charman, 2017, ACS medicinal chemistry letters.

Characterization of Novel Antimalarial Compound ACT-451840: Preclinical Assessment of Activity and Dose–Efficacy Modeling

R. Price, D. Fidock, R. Sinden, 2016, PLoS medicine.

Novel Inhibitors of Plasmodium falciparum Dihydroorotate Dehydrogenase with Anti-malarial Activity in the Mouse Model*

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3-Hydroxy-N'-arylidenepropanehydrazonamides with Halo-Substituted Phenanthrene Scaffolds Cure P. berghei Infected Mice When Administered Perorally.

E. Winzeler, S. Meister, B. Mordmüller, 2017, Journal of medicinal chemistry.

Blood schizontocidal and gametocytocidal activity of 3-hydroxy-N'-arylidenepropanehydrazonamides: a new class of antiplasmodial compounds.

B. Mordmüller, K. Kuna, W. Frank, 2014, Journal of medicinal chemistry.

Antimalarial activity of N-alkyl amine, carboxamide, sulfonamide, and urea derivatives of a dispiro-1,2,4-trioxolane piperidine.

J. Chollet, S. Charman, W. Charman, 2006, Bioorganic & medicinal chemistry letters.

Antimalarial Pyrido[1,2- a]benzimidazole Derivatives with Mannich Base Side Chains: Synthesis, Pharmacological Evaluation, and Reactive Metabolite Trapping Studies.

K. Chibale, John Okombo, G. Dziwornu, 2019, ACS infectious diseases.

Identification and In-Vitro ADME Assessment of a Series of Novel Anti-Malarial Agents Suitable for Hit-to-Lead Chemistry.

V. Avery, Chris D. Edlin, J. Bryans, 2012, ACS medicinal chemistry letters.

Identification of New Human Malaria Parasite Plasmodium falciparum Dihydroorotate Dehydrogenase Inhibitors by Pharmacophore and Structure-Based Virtual Screening

Margaret A. Phillips, Kelly Chibale, Sergio Wittlin, 2016, J. Chem. Inf. Model..

Monoclonal Antibodies That Recognize the Alkylation Signature of Antimalarial Ozonides OZ277 (Arterolane) and OZ439 (Artefenomel)

O. Biehlmaier, P. Mäser, H. Matile, 2015, ACS infectious diseases.

Probing the Antimalarial Mechanism of Artemisinin and OZ277 (Arterolane) with Nonperoxidic Isosteres and Nitroxyl Radicals

Yuxiang Dong, J. Vennerstrom, S. Wittlin, 2009, Antimicrobial Agents and Chemotherapy.

In vitro and in vivo interaction of synthetic peroxide RBx11160 (OZ277) with piperaquine in Plasmodium models.

J. Chollet, S. Wittlin, J. Santo-Tomas, 2007, Experimental parasitology.

Mechanism of Antimalarial Action of the Synthetic Trioxolane RBX11160 (OZ277)

S. Krishna, Leyla Y. Bustamante, A. Uhlemann, 2006, Antimicrobial Agents and Chemotherapy.

3D-QSAR Modeling and Synthesis of New Fusidic Acid Derivatives as Antiplasmodial Agents

Sergio Wittlin, Elumalai Pavadai, Kelly Chibale, 2018, J. Chem. Inf. Model..

Probing the Peroxycarbenium [3+2] Cycloaddition Reactions with 1,2-Disubstituted Ethylenes: Results and Insights.

S. Wittlin, Yikang Wu, Ze‐Jun Xu, 2017, Chemistry.

A pyridyl-furan series developed from Open Global Health Library blocks red blood cell invasion and protein trafficking in Plasmodium falciparum through potential inhibition of the parasite’s PI4KIIIb enzyme

P. Gilson, A. Barry, B. Crabb, 2023, bioRxiv.

In vitro assessment of the pharmacodynamic properties of DB75, piperaquine, OZ277 and OZ401 in cultures of Plasmodium falciparum.

R. Brun, H. Matile, S. Wittlin, 2008, The Journal of antimicrobial chemotherapy.

Cytochrome P450-Mediated Metabolism and CYP Inhibition for the Synthetic Peroxide Antimalarial OZ439.

David M. Shackleford, S. Charman, Qingjie Zhao, 2021, ACS infectious diseases.

Lead optimization of a pyrrole-based dihydroorotate dehydrogenase inhibitor series for the treatment of Malaria.

David M. Shackleford, P. Rathod, John White, 2020, Journal of medicinal chemistry.

Stochastic protein alkylation by antimalarial peroxides.

Remo S. Schmidt, P. Mäser, H. Matile, 2019, ACS infectious diseases.

Two successful decades of Swiss collaborations to develop new anti-malarials

M. Tanner, R. Hooft van Huijsduijnen, T. Wells, 2019, Malaria Journal.

Characterization of the two major CYP450 metabolites of ozonide (1,2,4-trioxolane) OZ277.

A. Ruf, S. Charman, W. Charman, 2008, Bioorganic & medicinal chemistry letters.

In vitro assessment of the pharmacodynamic properties and the partitioning of OZ277/RBx-11160 in cultures of Plasmodium falciparum.

S. Charman, R. Brun, H. Matile, 2006, The Journal of antimicrobial chemotherapy.

The comparative antimalarial properties of weak base and neutral synthetic ozonides.

J. Chollet, S. Charman, W. Charman, 2010, Bioorganic & medicinal chemistry letters.

Effect of functional group polarity on the antimalarial activity of spiro and dispiro-1,2,4-trioxolanes.

J. Chollet, S. Charman, W. Charman, 2006, Bioorganic & medicinal chemistry.

Diaryl Ureas as an Antiprotozoal Chemotype.

P. Davis, M. Kaiser, J. Vennerstrom, 2021, ACS infectious diseases.

Anti-malarial ozonides OZ439 and OZ609 tested at clinically relevant compound exposure parameters in a novel ring-stage survival assay

P. Mäser, D. Leroy, S. Wittlin, 2019, Malaria Journal.

In vitro interaction of artemisinin derivatives or the fully synthetic peroxidic anti-malarial OZ277 with thapsigargin in Plasmodium falciparum strains

R. Brun, S. Wittlin, O. Abiodun, 2013, Malaria Journal.

Antimalarial benzoheterocyclic 4-aminoquinolines: Structure-activity relationship, in vivo evaluation, mechanistic and bioactivation studies.

K. Chibale, T. Egan, C. Masimirembwa, 2015, Bioorganic & medicinal chemistry.

Resistance Signals using Multidrug-Resistant Plasmodium falciparum

S. Oliver, E. Bilsland, T. Egan, 2014 .

Synthesis and in vitro antiprotozoal activities of water-soluble, inexpensive 3,7-bis(dialkylamino)phenoxazin-5-ium derivatives.

J. Ge, R. Brun, M. Ihara, 2008, Journal of medicinal chemistry.

The Parasite Reduction Ratio (PRR) Assay Version 2: Standardized Assessment of Plasmodium falciparum Viability after Antimalarial Treatment In Vitro

F. Gamo, P. Mäser, D. Leroy, 2023, Pharmaceuticals.

Corrigendum: A novel multiple-stage antimalarial agent that inhibits protein synthesis

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A new double-antibody sandwich ELISA targeting Plasmodium falciparum aldolase to evaluate anti-malarial drug sensitivity

R. Brun, H. Matile, S. Wittlin, 2009, Malaria Journal.

Potent Antimalarials with Development Potential Identified by Structure-Guided Computational Optimization of a Pyrrole-Based Dihydroorotate Dehydrogenase Inhibitor Series.

David M. Shackleford, E. Winzeler, P. Rathod, 2021, Journal of medicinal chemistry.

Novel synthetic route for antimalarial benzo[a]phenoxazine derivative SSJ-183 and two active metabolites.

J. Ge, R. Brun, M. Ihara, 2014, Bioorganic & medicinal chemistry.

Evaluation of 4-Amino 2-Anilinoquinazolines against Plasmodium and Other Apicomplexan Parasites In Vitro and in a P. falciparum Humanized NOD-scid IL2Rγnull Mouse Model of Malaria

Christopher J. Tonkin, A. Cowman, F. Gamo, 2018, Antimicrobial Agents and Chemotherapy.

Compounds Structurally Related to Ellagic Acid Show Improved Antiplasmodial Activity

K. Fritz-Wolf, S. Rahlfs, K. Becker, 2008, Antimicrobial Agents and Chemotherapy.

Author Correction: Arylmethylamino steroids as antiparasitic agents

S. Rahlfs, K. Becker, E. Davioud‐Charvet, 2019, Nature Communications.

One-step purification of cathepsin D by affinity chromatography using immobilized propeptide sequences.

D. Stover, S. Wittlin, J. Rösel, 1998, European journal of biochemistry.

A Pyridyl-Furan Series Developed from the Open Global Health Library Block Red Blood Cell Invasion and Protein Trafficking in Plasmodium falciparum through Potential Inhibition of the Parasite’s PI4KIIIB Enzyme

P. Gilson, M. Delves, A. Barry, 2023, ACS infectious diseases.

Benzo[b]quinolizinium Derivatives Have a Strong Antimalarial Activity and Inhibit Indoleamine Dioxygenase

S. Rahlfs, K. Becker, H. Ihmels, 2015, Antimicrobial Agents and Chemotherapy.

Novel orally active antimalarial thiazoles.

K. Chibale, M. Witty, S. Charman, 2011, Journal of medicinal chemistry.

A long-duration dihydroorotate dehydrogenase inhibitor (DSM265) for prevention and treatment of malaria

Farah El Mazouni, T. Laird, P. Rathod, 2015, Science Translational Medicine.

Antimalarial activity of novel pyrrolizidinyl derivatives of 4-aminoquinoline.

S. Parapini, A. Sparatore, D. Taramelli, 2008, Bioorganic & Medicinal Chemistry Letters.

Antimalarial activity of novel pyrrolizidinyl derivatives of 4-aminoquinolines

S. Romeo, S. Parapini, A. Sparatore, 2006 .

Comparative Ex Vivo Activity of Novel Endoperoxides in Multidrug-Resistant Plasmodium falciparum and P. vivax

R. Price, E. Kenangalem, N. Anstey, 2012, Antimicrobial Agents and Chemotherapy.

Fast-Killing Tyrosine Amide ((S)-SW228703) with Blood- and Liver-Stage Antimalarial Activity Associated with the Cyclic Amine Resistance Locus (PfCARL).

E. Winzeler, M. Phillips, F. Gamo, 2023, ACS infectious diseases.

Identification and Profiling of a Novel Diazaspiro[3.4]octane Chemical Series Active against Multiple Stages of the Human Malaria Parasite Plasmodium falciparum and Optimization Efforts.

E. Winzeler, K. Chibale, Dale Taylor, 2021, Journal of medicinal chemistry.

On-target, dual aminopeptidase inhibition provides cross-species antimalarial activity

J. Marfurt, T. D. de Koning-Ward, S. Charman, 2024, mBio.

The Plasmodium Lactate/H+ Transporter PfFNT Is Essential and Druggable In Vivo

E. Beitz, T. Spielmann, S. Wittlin, 2023, Antimicrobial agents and chemotherapy.

Exploring a Tetrahydroquinoline Antimalarial Hit from the Medicines for Malaria Pathogen Box and Identification of its Mode of Resistance as PfeEF2

E. Winzeler, D. Fidock, F. Gamo, 2022, ChemMedChem.

Compounds Structurally Related to Ellagic Acid Show Improved Antiplasmodial Activity

K. Fritz-Wolf, S. Rahlfs, K. Becker, 2008, Antimicrobial Agents and Chemotherapy.

Antimalarial benzoheterocyclic 4-aminoquinolines: Structure-activity relationship, in vivo evaluation, mechanistic and bioactivation studies.

K. Chibale, T. Egan, C. Masimirembwa, 2015, Bioorganic & medicinal chemistry.

Discovery and Characterization of Potent, Efficacious, Orally Available Antimalarial Plasmepsin X Inhibitors and Preclinical Safety Assessment of UCB7362

Richard D. Taylor, D. Goldberg, A. Cowman, 2022, Journal of medicinal chemistry.

Probing the Antimalarial Mechanism of Artemisinin and OZ277 (Arterolane) with Nonperoxidic Isosteres and Nitroxyl Radicals

Yuxiang Dong, J. Vennerstrom, S. Wittlin, 2009, Antimicrobial Agents and Chemotherapy.

In vitro susceptibility of P. falciparum populations from Colombia and Tanzania to a new synthetic peroxide (OZ277).

R. Brun, H. Matile, V. Mayagaya, 2007, The American journal of tropical medicine and hygiene.

Chemoproteomics validates selective targeting of Plasmodium M1 alanyl aminopeptidase as an antimalarial strategy

G. Siddiqui, Sandra Duffy, N. Drinkwater, 2024, Research square.

Identification of potent and reversible piperidine carboxamides that are species-selective orally active proteasome inhibitors to treat malaria.

David M. Shackleford, D. Fidock, S. Charman, 2024, Cell chemical biology.

Incomplete Plasmodium falciparum growth inhibition following piperaquine treatment translates into increased parasite viability in the in vitro parasite reduction ratio assay

S. Wittlin, Bálint Tamási, C. Scheurer, 2024, Frontiers in cellular and infection microbiology.