J. Smaill

发表

Tyrosine kinase inhibitors. 15. 4-(Phenylamino)quinazoline and 4-(phenylamino)pyrido[d]pyrimidine acrylamides as irreversible inhibitors of the ATP binding site of the epidermal growth factor receptor.

W. Denny, G. Rewcastle, A. Bridges, 1999, Journal of medicinal chemistry.

The Horner-Wadsworth-Emmons Reaction in Natural Products Synthesis: Expedient Construction of Complex (E)-Enones Using Barium Hydroxide

J. Smaill, K. Yeung, I. Paterson, 1993 .

Selectively Targeting Tumor Hypoxia With the Hypoxia-Activated Prodrug CP-506

P. Lambin, L. Dubois, A. Jochems, 2021, Molecular Cancer Therapeutics.

Evaluating the abilities of diverse nitroaromatic prodrug metabolites to exit a model Gram negative vector for bacterial‐directed enzyme‐prodrug therapy

J. Smaill, J. Copp, D. Ackerley, 2018, Biochemical pharmacology.

Creation and screening of a multi-family bacterial oxidoreductase library to discover novel nitroreductases that efficiently activate the bioreductive prodrugs CB1954 and PR-104A.

W. Denny, J. Smaill, G. Prosser, 2013, Biochemical pharmacology.

Interrogation of the Structure–Activity Relationship of a Lipophilic Nitroaromatic Prodrug Series Designed for Cancer Gene Therapy Applications

J. Smaill, J. Copp, D. Ackerley, 2022, Pharmaceuticals.

Binding mode of the breakthrough inhibitor AZD9291 to epidermal growth factor receptor revealed.

J. Smaill, J. Flanagan, M. McKeage, 2015, Journal of structural biology.

Fibroblast Growth Factor Receptor 4 (FGFR4) Selective Inhibitors as Hepatocellular Carcinoma Therapy: Advances and Prospects.

J. Smaill, Xiaoyun Lu, A. Patterson, 2018, Journal of medicinal chemistry.

Restoring Tumour Selectivity of the Bioreductive Prodrug PR-104 by Developing an Analogue Resistant to Aerobic Metabolism by Human Aldo-Keto Reductase 1C3

J. Smaill, G. Prosser, G. Dachs, 2021, Pharmaceuticals.

Tyrosine kinase inhibitors. 19. 6-Alkynamides of 4-anilinoquinazolines and 4-anilinopyrido[3,4-d]pyrimidines as irreversible inhibitors of the erbB family of tyrosine kinase receptors.

P. Ellis, W. Denny, A. Bridges, 2006, Journal of medicinal chemistry.

The Flavin Reductase MsuE Is a Novel Nitroreductase that Can Efficiently Activate Two Promising Next-Generation Prodrugs for Gene-Directed Enzyme Prodrug Therapy

J. Smaill, J. Copp, D. Ackerley, 2013, Cancers.

Prototyping kinase inhibitor-cytotoxin anticancer mutual prodrugs activated by tumour hypoxia: A chemical proof of concept study.

J. Smaill, R. Anderson, M. Kelso, 2019, Bioorganic & medicinal chemistry letters.

Selectively Targeting Tumor Hypoxia With the Hypoxia-Activated Prodrug CP-506

P. Lambin, L. Dubois, A. Jochems, 2021, Molecular Cancer Therapeutics.

Specific, irreversible inactivation of the epidermal growth factor receptor and erbB2, by a new class of tyrosine kinase inhibitor.

W. Denny, A. Doherty, A. Bridges, 1998, Proceedings of the National Academy of Sciences of the United States of America.

Improved Strategy for the Synthesis of the Anticancer Agent Culicinin D

J. Smaill, Sung‐Hyun Yang, M. Brimble, 2015 .

Discovery of Isoform-Selective Akt3 Degraders Overcoming Osimertinib-Induced Resistance in Non-Small Cell Lung Cancer Cells.

J. Smaill, Liang Chen, A. Patterson, 2022, Journal of medicinal chemistry.

The 1.65 Å resolution structure of the complex of AZD4547 with the kinase domain of FGFR1 displays exquisite molecular recognition.

J. Smaill, A. Patterson, Y. Yosaatmadja, 2015, Acta crystallographica. Section D, Biological crystallography.

Investigation of Covalent Warheads in the Design of 2-Aminopyrimidine-based FGFR4 Inhibitors.

J. Smaill, Yongheng Chen, Xiaoyun Lu, 2021, ACS medicinal chemistry letters.

Synthesis and antiproliferative activity of C- and N-terminal analogues of culicinin D.

J. Smaill, M. Brimble, P. Harris, 2020, Bioorganic & medicinal chemistry letters.

Advancing Clostridia to Clinical Trial: Past Lessons and Recent Progress

P. Lambin, L. Dubois, J. Smaill, 2016, Cancers.

Discovery and evaluation of Escherichia coli nitroreductases that activate the anti-cancer prodrug CB1954.

W. Wilson, J. Smaill, G. Prosser, 2010, Biochemical pharmacology.

The synthesis and biological evaluation of novel series of nitrile-containing fluoroquinolones as antibacterial agents.

W. Denny, S. Hagen, J. Smaill, 2007, Bioorganic & medicinal chemistry letters.

Synthesis and cytotoxicity of pyranonaphthoquinone natural product analogues under bioreductive conditions.

J. Smaill, M. Brimble, S. Jamieson, 2013, Bioorganic & medicinal chemistry.

2,4-Diarylamino-pyrimidines as kinase inhibitors co-targeting IGF1R and EGFR(L⁸⁵⁸R/T⁷⁹⁰M).

J. Smaill, Jian Ding, Lin-jiang Tong, 2015, Bioorganic & medicinal chemistry letters.

Synthesis and structure-activity relationships of soluble 8-substituted 4-(2-chlorophenyl)-9-hydroxypyrrolo[3,4-c]carbazole-1,3(2H,6H)-diones as inhibitors of the Wee1 and Chk1 checkpoint kinases.

W. Denny, E. Baker, A. M. Thompson, 2008, Bioorganic & medicinal chemistry letters.

Structure-activity relationships for 2-anilino-6-phenylpyrido[2,3-d]pyrimidin-7(8H)-ones as inhibitors of the cellular checkpoint kinase Wee1.

W. Denny, G. Rewcastle, A. Kraker, 2005, Bioorganic & medicinal chemistry letters.

Tyrosine kinase inhibitors. 17. Irreversible inhibitors of the epidermal growth factor receptor: 4-(phenylamino)quinazoline- and 4-(phenylamino)pyrido[3,2-d]pyrimidine-6-acrylamides bearing additional solubilizing functions.

O. H. Chan, W. Denny, G. Rewcastle, 2000, Journal of medicinal chemistry.

Tyrosine Kinase Inhibitors. 20. Optimization of Substituted Quinazoline and Pyrido[3,4-d]pyrimidine Derivatives as Orally Active, Irreversible Inhibitors of the Epidermal Growth Factor Receptor Family.

J. A. Spicer, P. Ellis, W. Denny, 2016, Journal of medicinal chemistry.

Studies in biomimetic polyether synthesis: Construction of an ABCD-ring subunit of etheromycin using polyepoxide cascade cyclisations.

J. Smaill, I. Paterson, R. Tillyer, 1993 .

N-(3-Ethynyl-2,4-difluorophenyl)sulfonamide Derivatives as Selective Raf Inhibitors.

Yong Xu, J. Smaill, Donghai Wu, 2015, ACS medicinal chemistry letters.

4-Phenylpyrrolo[3,4-c]carbazole-1,3(2H,6H)-dione inhibitors of the checkpoint kinase Wee1. Structure-activity relationships for chromophore modification and phenyl ring substitution.

Daniel F Ortwine, Elizabeth A Lunney, W. Denny, 2006, Journal of medicinal chemistry.

2-Aminopyrimidine Derivatives as New Selective Fibroblast Growth Factor Receptor 4 (FGFR4) Inhibitors.

Yong Xu, J. Smaill, Xiaoyun Lu, 2017, ACS medicinal chemistry letters.

Zinc Finger Nuclease Knock-out of NADPH:Cytochrome P450 Oxidoreductase (POR) in Human Tumor Cell Lines Demonstrates That Hypoxia-activated Prodrugs Differ in POR Dependence*

W. Wilson, J. Smaill, F. Pruijn, 2013, The Journal of Biological Chemistry.

Effect of POR knockout on hypoxic prodrug activation

W. Wilson, J. Smaill, F. Pruijn, 2013 .

Use of an optimised enzyme/prodrug combination for Clostridia directed enzyme prodrug therapy induces a significant growth delay in necrotic tumours

P. Lambin, L. Dubois, J. Smaill, 2021, Cancer Gene Therapy.

E. coli nitroreductase NfsA is a reporter gene for non-invasive PET imaging in cancer gene therapy applications

P. Lambin, L. Dubois, J. Smaill, 2020, Theranostics.

Rational design of an AKR1C3-resistant analog of PR-104 for enzyme-prodrug therapy.

J. Smaill, J. Flanagan, J. Copp, 2016, Biochemical pharmacology.

Rational design of an AKR 1 C 3-resistant analog of PR-104 for enzyme-prodrug therapy

J. Smaill, J. Flanagan, J. Copp, 2016 .

The nitroreductase prodrug SN 28343 enhances the potency of systemically administered armed oncolytic adenovirus ONYX-411NTR

W. Denny, W. Wilson, J. Smaill, 2007, Cancer Gene Therapy.

Nitroreductase gene-directed enzyme prodrug therapy: insights and advances toward clinical utility.

J. Smaill, J. Copp, M. Rich, 2015, The Biochemical journal.

Tarloxotinib Is a Hypoxia-Activated Pan-HER Kinase Inhibitor Active Against a Broad Range of HER-Family Oncogenes

Chul Kim, R. Doebele, J. Smaill, 2020, Clinical Cancer Research.

TANK-binding kinase 1 (TBK1): an emerging therapeutic target for drug discovery.

J. Smaill, S. Xiang, Xiaoyun Lu, 2021, Drug discovery today.

New Promise and Opportunities for Allosteric Kinase Inhibitors.

J. Smaill, Xiaoyun Lu, Ke Ding, 2019, Angewandte Chemie.

Tumour Hypoxia-Mediated Immunosuppression: Mechanisms and Therapeutic Approaches to Improve Cancer Immunotherapy

J. Smaill, I. Hermans, A. Patterson, 2021, Cells.

Small-Molecule Inhibitors Directly Targeting KRAS as Anticancer Therapeutics.

J. Smaill, Xiaoyun Lu, Ke Ding, 2020, Journal of medicinal chemistry.

Targeting EGFRL858R/T790M and EGFRL858R/T790M/C797S resistance mutations in NSCLC: Current developments in medicinal chemistry

J. Smaill, Xiaoyun Lu, Ke Ding, 2018, Medicinal research reviews.

1-Benzyl-4-phenyl-1H-1,2,3-triazoles improve the transcriptional functions of estrogen-related receptor γ and promote the browning of white adipose.

Yong Xu, J. Smaill, Donghai Wu, 2015, Bioorganic & medicinal chemistry.

TAS-120 cancer target binding; defining reactivity and revealing the first FGFR1 irreversible structure.

J. Smaill, M. Middleditch, A. Patterson, 2019 .

TAS‐120 Cancer Target Binding: Defining Reactivity and Revealing the First Fibroblast Growth Factor Receptor 1 (FGFR1) Irreversible Structure

J. Smaill, M. Middleditch, A. Patterson, 2019, ChemMedChem.

The Discovery of Dacomitinib, a Potent Irreversible EGFR Inhibitor

J. Smaill, Jessica E. Reed, 2016 .

Medicinal Chemistry Strategies for the Development of Kinase Inhibitors Targeting Point Mutations.

J. Smaill, Xiaoyun Lu, Ke Ding, 2020, Journal of medicinal chemistry.

2-Oxo-3, 4-dihydropyrimido[4, 5-d]pyrimidinyl derivatives as new irreversible pan fibroblast growth factor receptor (FGFR) inhibitors.

Yong Xu, J. Smaill, Xiaoyun Lu, 2017, European journal of medicinal chemistry.

Design, Synthesis, and Biological Evaluation of 5-Formyl-pyrrolo[3,2-b]pyridine-3-carboxamides as New Selective, Potent, and Reversible-Covalent FGFR4 Inhibitors.

J. Smaill, Zheng-chao Tu, A. Patterson, 2022, Journal of medicinal chemistry.

Rotational Freedom, Steric Hindrance, and Protein Dynamics Explain BLU554 Selectivity for the Hinge Cysteine of FGFR4.

J. Smaill, Xiaoyun Lu, M. Middleditch, 2019, ACS medicinal chemistry letters.

Discovery of Cysteine-targeting Covalent Protein Kinase Inhibitors.

J. Smaill, Xiaoyun Lu, A. Patterson, 2021, Journal of medicinal chemistry.

Engineering a Multifunctional Nitroreductase for Improved Activation of Prodrugs and PET Probes for Cancer Gene Therapy.

J. Smaill, J. Flanagan, J. Copp, 2017, Cell chemical biology.

Mono- and dysfunctional nitrogen mustard analogues of the DNA minor groove binder pibenzimol. Synthesis, cytotoxicity and interaction with DNA.

W. Denny, J. Smaill, J. Fan, 1998, Anti-cancer drug design.

A novel fluorometric assay for aldo-keto reductase 1C3 predicts metabolic activation of the nitrogen mustard prodrug PR-104A in human leukaemia cells.

S. Bohlander, M. Konopleva, W. Wilson, 2014, Biochemical pharmacology.

Subcellular Location of Tirapazamine Reduction Dramatically Affects Aerobic but Not Anoxic Cytotoxicity

Su Jung Lee, W. Denny, W. Wilson, 2020, Molecules.

Design, Synthesis and In-Vitro Biological Evaluation of Antofine and Tylophorine Prodrugs as Hypoxia-Targeted Anticancer Agents

J. Smaill, P. Fischer, Ashraf N. Abdalla, 2021, Molecules.

Alanine scan-guided synthesis and biological evaluation of analogues of culicinin D, a potent anticancer peptaibol.

J. Smaill, M. Brimble, P. Harris, 2020, Bioorganic & medicinal chemistry letters.

Chinese Journal of Cancer

Dong-hai Wu, J. Smaill, K. Ding, 2022 .

Targeted mutagenesis of the Vibrio fischeri flavin reductase FRase I to improve activation of the anticancer prodrug CB1954.

J. Smaill, J. Copp, D. Ackerley, 2012, Biochemical pharmacology.

Pre-Clinical Activity of Novel Hypoxia-Activated FLT3 Inhibitors in FLT3-Mutated AML

M. Konopleva, J. Smaill, N. Daver, 2016 .

Hypoxia-activated prodrugs and (lack of) clinical progress: The need for hypoxia-based biomarker patient selection in phase III clinical trials

P. Lambin, L. Dubois, D. de Ruysscher, 2019, Clinical and translational radiation oncology.

Discovery and optimization of 1-(1H-indol-1-yl)ethanone derivatives as CBP/EP300 bromodomain inhibitors for the treatment of castration-resistant prostate cancer.

Cheng Zhang, Ke Ding, Donghai Wu, 2018, European journal of medicinal chemistry.

Abstract 4025: STEAP4 ISH and IHC diagnostics for Tarloxotinib activation in EGFR/HER2 mutant cancers

F. Hirsch, R. Doebele, J. Smaill, 2019, Clinical Research (Excluding Clinical Trials).

Tissue Pharmacokinetic Properties and Bystander Potential of Hypoxia-Activated Prodrug CP-506 by Agent-Based Modelling

J. Smaill, K. Hicks, A. Patterson, 2022, Frontiers in Pharmacology.

Bioreductive prodrug PR-104 improves the tumour distribution and titre of the nitroreductase-armed oncolytic adenovirus ONYX-411NTR leading to therapeutic benefit

W. Wilson, J. Smaill, D. Singleton, 2021, Cancer Gene Therapy.

Bioreductive prodrug PR-104 improves the tumour distribution and titre of the nitroreductase-armed oncolytic adenovirus ONYX-411NTR leading to therapeutic benefit

W. Wilson, J. Smaill, Dan Li, 2021, Cancer Gene Therapy.

Design, Synthesis, and Biological Evaluation of Aminoindazole Derivatives as Highly Selective Covalent Inhibitors of Wild-Type and Gatekeeper Mutant FGFR4.

J. Smaill, Yongheng Chen, Xiaoyun Lu, 2022, Journal of medicinal chemistry.

Structural Mechanism and Inhibitors Targeting EGFR Exon 20 Insertion (Ex20ins) Mutations.

J. Smaill, Hao Chen, A. Patterson, 2023, Journal of medicinal chemistry.

Fourth-Generation Analogues of the Anticancer Peptaibol Culicinin D: Probing the Effects of Hydrophobicity and Halogenation on Cytotoxicity

J. Smaill, M. Brimble, P. Harris, 2021, Synthesis.

Synthesis and structure-activity relationships of N-6 substituted analogues of 9-hydroxy-4-phenylpyrrolo[3,4-c]carbazole-1,3(2H,6H)-diones as inhibitors of Wee1 and Chk1 checkpoint kinases.

W. Denny, E. Lunney, E. Baker, 2008, European journal of medicinal chemistry.

Binding mode of the breakthrough inhibitor AZD9291 to epidermal growth factor receptor revealed.

J. Smaill, J. Flanagan, M. McKeage, 2015, Journal of structural biology.

Tyrosine kinase inhibitors. 18. 6-Substituted 4-anilinoquinazolines and 4-anilinopyrido[3,4-d]pyrimidines as soluble, irreversible inhibitors of the epidermal growth factor receptor.

J. Smaill, W A Denny, J M Nelson, 2001, Journal of medicinal chemistry.

Engineering Escherichia coli NfsB to activate a hypoxia-resistant analog of the PET probe EF5 to enable non-invasive imaging during enzyme-prodrug therapy.

J. Smaill, J. Flanagan, J. Copp, 2019, Biochemistry.

Discovery of 6-Formylpyridyl Urea Derivatives as Potent Reversible-Covalent Fibroblast Growth Factor Receptor 4 Inhibitors with Improved Anti-Hepatocellular Carcinoma Activity.

J. Smaill, A. Patterson, Xiaojuan Chen, 2024, Journal of medicinal chemistry.

53 Pyrrolo[3,4-c]carbazole-1,3-dione inhibitors of the G2/M checkpoint kinase wee1

W. Denny, A. M. Thompson, A. Kraker, 2004 .

Toward a high-throughput screening platform for directed evolution of enzymes that activate genotoxic prodrugs.

J. Smaill, J. Copp, M. Rich, 2014, Protein engineering, design & selection : PEDS.

Abstract A157: Antitumor activity of tarloxotinib, a hypoxia-activated EGFR TKI, in patient-derived lung cancer cell lines harboring EGFR exon 20 insertions

R. Doebele, J. Smaill, A. Le, 2018 .

FGFR4 complex with N-(3-chloro-2-((5-((2,6-dichloro-3,5-dimethoxybenzyl)oxy)pyrimidin-2-yl)amino)-5-fluorophenyl)acrylamide

J. Smaill, Xiaoyun Lu, A. Patterson, 2019 .