Chiara Borsari

发表

Comparing Drug Images and Repurposing Drugs with BioGPS and FLAPdock: The Thymidylate Synthase Case

Francesca Spyrakis, Maria Paola Costi, Gabriele Cruciani, 2016, ChemMedChem.

Scouting new sigma receptor ligands: Synthesis, pharmacological evaluation and molecular modeling of 1,3-dioxolane-based structures and derivatives.

A. Prandi, S. Franchini, P. Fossa, 2016, European journal of medicinal chemistry.

Target-based approaches for the discovery of new antimycobacterial drugs.

Maria Paola Costi, Chiara Borsari, S. Ferrari, 2017, Drug discovery today.

Crassiflorone derivatives that inhibit Trypanosoma brucei glyceraldehyde-3-phosphate dehydrogenase (TbGAPDH) and Trypanosoma cruzi trypanothione reductase (TcTR) and display trypanocidal activity.

Maria Paola Costi, A. Cavalli, M. Bolognesi, 2017, European journal of medicinal chemistry.

Accelerating Drug Discovery Efforts for Trypanosomatidic Infections Using an Integrated Transnational Academic Drug Discovery Platform

Maria Paola Costi, R. Wade, M. Bolognesi, 2019, SLAS discovery : advancing life sciences R & D.

Excited-state intramolecular proton transfer in a bioactive flavonoid provides fluorescence observables for recognizing its engagement with target proteins

Maria Paola Costi, M. Caselli, G. Ponterini, 2019, Photochemical & photobiological sciences : Official journal of the European Photochemistry Association and the European Society for Photobiology.

Scalable, Economical, and Practical Synthesis of 4-(Difluoromethyl)pyridin-2-amine, a Key Intermediate for Lipid Kinase Inhibitors

M. Neuburger, M. Wymann, F. Beaufils, 2019, Organic Process Research & Development.

Two-drug trick to target the brain blocks toxicity in the body

M. Wymann, Chiara Borsari, 2022, Nature.

Chroman-4-One Derivatives Targeting Pteridine Reductase 1 and Showing Anti-Parasitic Activity

Maria Paola Costi, R. Wade, S. Gul, 2017, Molecules.

Identification of a 2,4-diaminopyrimidine scaffold targeting Trypanosoma brucei pteridine reductase 1 from the LIBRA compound library screening campaign.

Maria Paola Costi, A. Cavalli, M. Bolognesi, 2020, European journal of medicinal chemistry.

Structural Insights into the Development of Cycloguanil Derivatives as Trypanosoma brucei Pteridine-Reductase-1 Inhibitors.

Maria Paola Costi, S. Gul, S. Mangani, 2019, ACS infectious diseases.

Investigation of morpholine isosters for the development of a potent, selective and metabolically stable mTOR kinase inhibitor.

M. Wymann, F. Beaufils, C. Tarantelli, 2022, European journal of medicinal chemistry.

Second-generation tricyclic pyrimido-pyrrolo-oxazine mTOR inhibitor with predicted blood–brain barrier permeability

M. Wymann, Erhan Keles, M. Hamburger, 2021, RSC medicinal chemistry.

SAR Studies and Biological Characterization of a Chromen-4-one Derivative as an Anti-Trypanosoma brucei Agent.

Maria Paola Costi, S. Gul, G. Ponterini, 2019, ACS medicinal chemistry letters.

Designing Chimeric Molecules for Drug Discovery by Leveraging Chemical Biology

Maria Paola Costi, Darci J. Trader, Chiara Borsari, 2020, Journal of medicinal chemistry.

Discovery of a benzothiophene-flavonol halting miltefosine and antimonial drug resistance in Leishmania parasites through the application of medicinal chemistry, screening and genomics.

Maria Paola Costi, S. Gul, G. Ponterini, 2019, European journal of medicinal chemistry.

5-(4,6-Dimorpholino-1,3,5-triazin-2-yl)-4-(trifluoromethyl)pyridin-2-amine (PQR309), a Potent, Brain-Penetrant, Orally Bioavailable, Pan-Class I PI3K/mTOR Inhibitor as Clinical Candidate in Oncology.

J. Mestan, D. Fabbro, M. Zvelebil, 2017, Journal of medicinal chemistry.

Scaffolds and Biological Targets Avenue to Fight Against Drug Resistance in Leishmaniasis

Maria Paola Costi, N. Santarém, A. Cordeiro-da-Silva, 2018 .

A Conformational Restriction Strategy for the Identification of a Highly Selective Pyrimido-Pyrrolo-Oxazine mTOR Inhibitor.

D. Fabbro, M. Wymann, F. Beaufils, 2019, Journal of medicinal chemistry.

Rommie E. Amaro, M. Rathinaswamy, J. Burke, 2021, eLife.

Chemical and Structural Strategies to Selectively Target mTOR Kinase

M. Wymann, Chiara Borsari, M. De Pascale, 2021, ChemMedChem.

Rommie E. Amaro, M. Rathinaswamy, J. Burke, 2020, bioRxiv.

Profiling of Flavonol Derivatives for the Development of Antitrypanosomatidic Drugs.

Maria Paola Costi, R. Wade, S. Gul, 2016, Journal of medicinal chemistry.

Design, Synthesis and Antiparasitic Evaluation of Click Phospholipids

Maria Paola Costi, S. Gul, W. de Souza, 2021, Molecules.

Methoxylated 2'-hydroxychalcones as antiparasitic hit compounds.

Maria Paola Costi, S. Gul, L. Costantino, 2017, European journal of medicinal chemistry.

Covalent Proximity Scanning of a Distal Cysteine to Target PI3Kα

M. Gstaiger, J. Burke, M. Wymann, 2022, Journal of the American Chemical Society.

M. Rathinaswamy, R. Amaro, M. Wymann, 2021 .

Preclinical Development of PQR514, a Highly Potent PI3K Inhibitor Bearing a Difluoromethyl–Pyrimidine Moiety

Ivan V. Buslov, D. Fabbro, M. Wymann, 2019, ACS medicinal chemistry letters.

4-(Difluoromethyl)-5-(4-((3R,5S)-3,5-dimethylmorpholino)-6-((R)-3-methylmorpholino)-1,3,5-triazin-2-yl)pyridin-2-amine (PQR626), a Potent, Orally Available, and Brain-Penetrant mTOR Inhibitor for the Treatment of Neurological Disorders.

D. Fabbro, W. Löscher, M. Wymann, 2020, Journal of medicinal chemistry.

Role of Stereochemistry on the Biological Activity of Nature-Inspired 3-Br-Acivicin Isomers and Derivatives

S. Parapini, S. Bruno, C. Fattorusso, 2023, Molecules.

Virtual Screening and X-ray Crystallography Identify Non-Substrate Analog Inhibitors of Flavin-Dependent Thymidylate Synthase.

Maria Paola Costi, T. Blundell, G. Ponterini, 2016, Journal of medicinal chemistry.

Discovery and Preclinical Characterization of 5-[4,6-Bis({3-oxa-8-azabicyclo[3.2.1]octan-8-yl})-1,3,5-triazin-2-yl]-4-(difluoromethyl)pyridin-2-amine (PQR620), a Highly Potent and Selective mTORC1/2 Inhibitor for Cancer and Neurological Disorders.

D. Fabbro, M. Zvelebil, W. Löscher, 2018, Journal of medicinal chemistry.

Discovery of a spirocyclic 3-bromo-4,5-dihydroisoxazole covalent inhibitor of hGAPDH with antiproliferative activity against pancreatic cancer cells.

R. Pacchiana, M. Donadelli, S. Bruno, 2023, European journal of medicinal chemistry.

X-ray crystal structures of Enterococcus faecalis thymidylate synthase with folate binding site inhibitors.

S. Mangani, A. Catalano, C. Pozzi, 2016, European journal of medicinal chemistry.

( S)-4-(Difluoromethyl)-5-(4-(3-methylmorpholino)-6-morpholino-1,3,5-triazin-2-yl)pyridin-2-amine (PQR530), a Potent, Orally Bioavailable, and Brain-Penetrable Dual Inhibitor of Class I PI3K and mTOR Kinase.

D. Fabbro, J. Burke, M. Wymann, 2019, Journal of medicinal chemistry.

Design, Synthesis and Structure—Activity Relationships of a Phenotypic Small Library against Protozoan Infections

Maria Paola Costi, L. Piazzi, F. Belluti, 2017 .

Development of a Focused Library of Triazole‐Linked Privileged‐Structure‐Based Conjugates Leading to the Discovery of Novel Phenotypic Hits against Protozoan Parasitic Infections

Maria Paola Costi, L. Piazzi, F. Belluti, 2018, ChemMedChem.

The Facets of Diversity: The EFMC Perspective **

Y. Auberson, Chiara Borsari, K. Goncharenko, 2022, ChemMedChem.

Novel Dithiolane-Based Ligands Combining Sigma and NMDA Receptor Interactions as Potential Neuroprotective Agents.

S. Franchini, L. Brasili, R. Iacobazzi, 2020, ACS medicinal chemistry letters.

A high affinity pan-PI3K binding module supports selective targeted protein degradation of PI3Kα

S. Zhanybekova, Chiara Borsari, Dennis Gillingham, 2023, Chemical science.

Discovery of 1,3,4-Oxadiazole Derivatives as Broad-Spectrum Antiparasitic Agents.

S. Parapini, L. Tamborini, A. Altomare, 2024, ACS infectious diseases.

Boosting the Impact of EFMC Young Scientists Network Through the Creation of Working Groups.

Chiara Borsari, Laia Josa-Culleré, M. Mari, 2024, ChemMedChem.