Discovery of 1,4-dihydroindeno[1,2-c]pyrazoles as a novel class of potent and selective checkpoint kinase 1 inhibitors

Autor:	Hing L. Sham, Russell A. Judge, Akiyo Claiborne, Thomas J. Sowin, Haiying Zhang, Stephen L. Gwaltney, Nan-Horng Lin, Kent D. Stewart, Yunsong Tong, Chang Park, Saul H. Rosenberg, Peter Kovar, Zehan Chen, Wen-Zhen Gu, Robert B. Credo
Rok vydání:	2007
Předmět:	Models Molecular Magnetic Resonance Spectroscopy Stereochemistry High-throughput screening Clinical Biochemistry Drug Evaluation Preclinical Pharmaceutical Science Pyrazole Crystallography X-Ray Biochemistry Substrate Specificity chemistry.chemical_compound Drug Discovery medicine Humans CHEK1 Protein kinase A Protein Kinase Inhibitors Molecular Biology Cell Proliferation chemistry.chemical_classification biology Chemistry Cell growth Cell Cycle Organic Chemistry Drug Synergism Hydrogen Bonding Antineoplastic Agents Phytogenic Enzyme Enzyme inhibitor Checkpoint Kinase 1 biology.protein Pyrazoles Molecular Medicine Camptothecin Indicators and Reagents Protein Kinases HeLa Cells medicine.drug
Zdroj:	Bioorganic & Medicinal Chemistry. 15:2759-2767
ISSN:	0968-0896
DOI:	10.1016/j.bmc.2007.01.012
Popis:	A new class of checkpoint kinase 1 (CHK-1) inhibitors bearing a 1,4-dihydroindeno[1,2-c]pyrazole core was developed after initial hits from high throughput screening. The efficient hit-to-lead process was facilitated by X-ray crystallography and led to potent inhibitors (
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7ae47e5b591d4943cf0905bb26642807 https://doi.org/10.1016/j.bmc.2007.01.012 Zobrazit plný text záznamu Full Text from ScienceDirect