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Your search keyword '"Nicholas John Newcombe"' showing total 2 results
Start Over Author "Nicholas John Newcombe" Journal bioorganic & medicinal chemistry letters
2 results on '"Nicholas John Newcombe"'

1. Discovery of a novel class of triazolones as Checkpoint Kinase inhibitors—Hit to lead exploration

Author

Paul Lyne, Patrick Brassil, Ann White, Jason Breed, Mei Su, Dorin Toader, Yan Yu, Sonya Zabludoff, Jon Read, James W. Janetka, Chun Deng, Dingwei Yu, Vibha Oza, Susan Ashwell, Zheng Xiaolan, Nicholas John Newcombe, Candice Horn, Martin Pass, Peter J. H. Webborn, Ludo Otterbien, Heather Haye, Jay Ezhuthachan, Anna L Valentine, and Sian Roswell

Subjects
Models, Molecular, animal structures, High-throughput screening, genetic processes, Clinical Biochemistry, Pharmaceutical Science, Computational biology, Crystallography, X-Ray, environment and public health, Biochemistry, Structure-Activity Relationship, Drug Discovery, Structure–activity relationship, CHEK1, Protein kinase A, Protein Kinase Inhibitors, Molecular Biology, Kinase, Drug discovery, Chemistry, Organic Chemistry, Hit to lead, Triazoles, enzymes and coenzymes (carbohydrates), Checkpoint Kinase 1, Molecular Medicine, biological phenomena, cell phenomena, and immunity, Signal transduction, Protein Kinases
Abstract

Checkpoint Kinase-1 (Chk1, CHK1, CHEK1) is a Ser/Thr protein kinase that mediates cellular responses to DNA-damage. A novel class of Chk1 inhibitors, triazoloquinolones/triazolones (TZ's) was identified by high throughput screening. The optimization of these hits to provide a lead series is described.

Published
2010

2. Discovery of a novel class of 2-ureido thiophene carboxamide checkpoint kinase inhibitors

Author

Candice Horn, Martin Pass, James W. Janetka, Kevin Daly, Nicholas John Newcombe, Mei Su, Stephanie Springer, Stephanos Ioannidis, Paul Lyne, Patrick Brassil, Melissa Vasbinder, Dingwei Yu, Vibha Oza, Chun Deng, Lynsie Almeida, Dorin Toader, Sonya Zabludoff, Susan Ashwell, Yan Yu, Roberta E. Glynn, and Thomas Gero

Subjects
Stereochemistry, medicine.drug_class, Chemistry, Pharmaceutical, Clinical Biochemistry, Pharmaceutical Science, Apoptosis, Carboxamide, Thiophenes, environment and public health, Biochemistry, Inhibitory Concentration 50, chemistry.chemical_compound, Drug Discovery, medicine, Thiophene, Humans, Urea, CHEK1, Protein kinase A, Protein Kinase Inhibitors, Molecular Biology, chemistry.chemical_classification, Cyclin-dependent kinase 1, biology, Kinase, Phenyl Ethers, Cell Cycle, Organic Chemistry, Amides, Carbon, enzymes and coenzymes (carbohydrates), Enzyme, Models, Chemical, chemistry, Enzyme inhibitor, Drug Design, Checkpoint Kinase 1, biology.protein, Molecular Medicine, biological phenomena, cell phenomena, and immunity, Protein Kinases, DNA Damage
Abstract

Checkpoint kinase-1 (Chk1, CHEK1) is a Ser/Thr protein kinase that mediates the cellular response to DNA-damage. A novel class of 2-ureido thiophene carboxamide urea (TCU) Chk1 inhibitors is described. Inhibitors in this chemotype were optimized for cellular potency and selectivity over Cdk1.

Published
2008

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