Publications by authors named "Jeff B Smaill"

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Design, Synthesis and Biological Evaluation of 7-(1-Methyl-1-indole-3-yl)-5-pyrrolo[2,3-]pyrazine Derivatives as Novel Covalent pan-FGFR Inhibitors to Overcome Clinical Resistance.
Wuqing Deng, Xiaojuan Chen, Ling Yan, Shuang Xiang, Xiaojuan Song, Jeff B Smaill

J Med Chem· September 2025

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Discovery of 5-imidazole-3-methylbenz[d]isoxazole derivatives as potent and selective CBP/p300 bromodomain inhibitors for the treatment of acute myeloid leukemia.
Jian-Kang Hu, Xin Tang, Guo-Long Luo, Cheng Zhang, Tian-Bang Wu, Jeff B Smaill

Acta Pharmacol Sin· June 2025

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Optimization of Aminoindazole derivatives as highly selective covalent inhibitors for wild-type and mutant FGFR4.
Jing Guo, Xiaojuan Chen, Xiaofei Li, Xuan Wang, Min Shao, Jeff B Smaill

Bioorg Chem· June 2025

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Discovery of a Potent and Selective GSPT1 Molecular Glue Degrader for the Treatment of Castration-Resistant Prostate Cancer.
Hui Shen, Hongrui Xu, Weiqin Jin, Tianbang Wu, Jiankang Hu, Jeff B Smaill

J Med Chem· January 2025

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The third generation AKR1C3-activated prodrug, ACHM-025, eradicates disease in preclinical models of aggressive T-cell acute lymphoblastic leukemia.
Cara E Toscan, Hannah McCalmont, Amir Ashoorzadeh, Xiaojing Lin, Zhe Fu, Jeff B Smaill

Blood Cancer J· November 2024

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Structural Evaluation of a Nitroreductase Engineered for Improved Activation of the 5-Nitroimidazole PET Probe SN33623.
Abigail V Sharrock, Jeff S Mumm, Elsie M Williams, Narimantas Čėnas, Jeff B Smaill

Int J Mol Sci· June 2024

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Discovery of 6-Formylpyridyl Urea Derivatives as Potent Reversible-Covalent Fibroblast Growth Factor Receptor 4 Inhibitors with Improved Anti-Hepatocellular Carcinoma Activity.
Fang Yang, Qianmeng Lin, Xiaojuan Song, Huisi Huang, Xiaojuan Chen, Jeff B Smaill

J Med Chem· February 2024

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Design and Biological Evaluation of Piperazine-Bearing Nitrobenzamide Hypoxia/GDEPT Prodrugs: The Discovery of CP-506.
Amir Ashoorzadeh, Alexandra M Mowday, Maria R Abbattista, Christopher P Guise, Matthew R Bull, Jeff B Smaill

ACS Med Chem Lett· November 2023

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Structural Mechanism and Inhibitors Targeting EGFR Exon 20 Insertion (Ex20ins) Mutations.
Hao Chen, Shiliang Hu, Adam V Patterson, Jeff B Smaill, Ke Ding

J Med Chem· September 2023

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Rational Design of Covalent Kinase Inhibitors by an Integrated Computational Workflow (Kin-Cov).
Yang Zhou, Hang Yu, Anna Constance Vind, Lulu Kong, Yiling Liu, Jeff B Smaill

J Med Chem· June 2023

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Design, Synthesis, and Biological Evaluation of 5-Formyl-pyrrolo[3,2-]pyridine-3-carboxamides as New Selective, Potent, and Reversible-Covalent FGFR4 Inhibitors.
Fang Yang, Xiaojuan Chen, Xiaojuan Song, Raquel Ortega, Xiaojing Lin, Jeff B Smaill

J Med Chem· November 2022

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Discovery of Isoform-Selective Akt3 Degraders Overcoming Osimertinib-Induced Resistance in Non-Small Cell Lung Cancer Cells.
Fang Xu, Xin Zhang, Zhipeng Chen, Sheng He, Jing Guo, Jeff B Smaill

J Med Chem· October 2022

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Bioreductive prodrug PR-104 improves the tumour distribution and titre of the nitroreductase-armed oncolytic adenovirus ONYX-411 leading to therapeutic benefit.
Dean C Singleton, Alexandra M Mowday, Chris P Guise, Sophie P Syddall, Sally Y Bai, Jeff B Smaill

Cancer Gene Ther· July 2022

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Design, Synthesis, and Biological Evaluation of Aminoindazole Derivatives as Highly Selective Covalent Inhibitors of Wild-Type and Gatekeeper Mutant FGFR4.
Min Shao, Xiaojuan Chen, Fang Yang, Xiaojuan Song, Yang Zhou, Jeff B Smaill

J Med Chem· March 2022

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Use of an optimised enzyme/prodrug combination for Clostridia directed enzyme prodrug therapy induces a significant growth delay in necrotic tumours.
Alexandra M Mowday, Ludwig J Dubois, Aleksandra M Kubiak, Jasmine V E Chan-Hyams, Christopher P Guise, Jeff B Smaill

Cancer Gene Ther· February 2022

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Tissue Pharmacokinetic Properties and Bystander Potential of Hypoxia-Activated Prodrug CP-506 by Agent-Based Modelling.
Victoria Jackson-Patel, Emily Liu, Matthew R Bull, Amir Ashoorzadeh, Gib Bogle, Jeff B Smaill

Front Pharmacol· February 2022

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Interrogation of the Structure-Activity Relationship of a Lipophilic Nitroaromatic Prodrug Series Designed for Cancer Gene Therapy Applications.
Amir Ashoorzadeh, Alexandra M Mowday, Christopher P Guise, Shevan Silva, Matthew R Bull, Jeff B Smaill

Pharmaceuticals (Basel)· February 2022

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Discovery of Cysteine-targeting Covalent Protein Kinase Inhibitors.
Xiaoyun Lu, Jeff B Smaill, Adam V Patterson, Ke Ding

J Med Chem· January 2022

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Selectively Targeting Tumor Hypoxia With the Hypoxia-Activated Prodrug CP-506.
Alexander M A van der Wiel, Victoria Jackson-Patel, Raymon Niemans, Ala Yaromina, Emily Liu, Jeff B Smaill

Mol Cancer Ther· December 2021

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Restoring Tumour Selectivity of the Bioreductive Prodrug PR-104 by Developing an Analogue Resistant to Aerobic Metabolism by Human Aldo-Keto Reductase 1C3.
Maria R Abbattista, Amir Ashoorzadeh, Christopher P Guise, Alexandra M Mowday, Rituparna Mittra, Jeff B Smaill

Pharmaceuticals (Basel)· November 2021

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TANK-binding kinase 1 (TBK1): An emerging therapeutic target for drug discovery.
Shuang Xiang, Shukai Song, Haotian Tang, Jeff B Smaill, Aiqun Wang

Drug Discov Today· October 2021

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Design, Synthesis and In-Vitro Biological Evaluation of Antofine and Tylophorine Prodrugs as Hypoxia-Targeted Anticancer Agents.
Ziad Omran, Chris P Guise, Linwei Chen, Cyril Rauch, Ashraf N Abdalla, Jeff B Smaill

Molecules· June 2021

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Investigation of Covalent Warheads in the Design of 2-Aminopyrimidine-based FGFR4 Inhibitors.
Wuqing Deng, Xiaojuan Chen, Kaili Jiang, Xiaojuan Song, Minhao Huang, Jeff B Smaill

ACS Med Chem Lett· April 2021

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Tumour Hypoxia-Mediated Immunosuppression: Mechanisms and Therapeutic Approaches to Improve Cancer Immunotherapy.
Zhe Fu, Alexandra M Mowday, Jeff B Smaill, Ian F Hermans, Adam V Patterson

Cells· April 2021

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Tarloxotinib Is a Hypoxia-Activated Pan-HER Kinase Inhibitor Active Against a Broad Range of HER-Family Oncogenes.
Adriana Estrada-Bernal, Anh T Le, Andrea E Doak, Vijaya G Tirunagaru, Shevan Silva, Jeff B Smaill

Clin Cancer Res· March 2021

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