4-(1H-Indazol-5-yl)-6-phenylpyrimidin-2(1H)-one analogs as potent CDC7 inhibitors

Autor:	Weiping Jia, Walter Annette O, Cornelia Bellamacina, Song Lin, Mika Lindvall, Asha Yabannavar, Cynthia M. Shafer, Thomas G. Gesner
Rok vydání:	2008
Předmět:	Indazoles Molecular model Stereochemistry Chemistry Pharmaceutical Clinical Biochemistry Molecular Conformation Pharmaceutical Science Cell Cycle Proteins Pyrimidinones Non-specific serine/threonine protein kinase Protein Serine-Threonine Kinases Biochemistry Inhibitory Concentration 50 Structure-Activity Relationship chemistry.chemical_compound Drug Discovery Humans Pyrimidone Enzyme Inhibitors Molecular Biology chemistry.chemical_classification Indazole Binding Sites Molecular Structure Bicyclic molecule biology Organic Chemistry Enzyme Models Chemical chemistry Enzyme inhibitor Drug Design Benzene derivatives biology.protein Molecular Medicine Caco-2 Cells
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 18:4482-4485
ISSN:	0960-894X
DOI:	10.1016/j.bmcl.2008.07.061
Popis:	A series of 4-(4-hydroxyphenyl)-6-phenylpyrimidin-2(1H)-ones were identified by HTS as inhibitors of CDC7. Molecular modeling and medicinal chemistry techniques were employed to explore the SAR for this series with a focus on removing potential metabolic liabilities and improving cellular potency.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::217a9c193aa9d3505e5bd2a9da18d9e6 https://doi.org/10.1016/j.bmcl.2008.07.061 Zobrazit plný text záznamu Full Text from ScienceDirect