N-(4-(6,7-Disubstituted-quinolin-4-yloxy)-3-fluorophenyl)-2-oxo-3-phenylimidazolidine-1-carboxamides: a novel series of dual c-Met/VEGFR2 receptor tyrosine kinase inhibitors

Autor:	Carole Beaulieu, Marja Dubay, Jeffrey M. Besterman, Stephane Raeppel, Jubrail Rahil, Nancy Z. Zhou, Ian Chute, Arkadii Vaisburg, Lijie Zhan, Isabelle Dupont, Hannah Nguyen, Ljubomir Isakovic, James Wang, Robert Deziel, Stephen William Claridge, Frédéric Gaudette, A. Robert MacLeod, Normand Beaulieu, Hélène Ste-Croix, Marie-France Robert, Sylvain Lefebvre, Oscar Mario Saavedra, Michael Mannion, Franck Raeppel
Rok vydání:	2009
Předmět:	Models Molecular C-Met medicine.drug_class Stereochemistry Clinical Biochemistry Pharmaceutical Science Carboxamide Antineoplastic Agents Biochemistry Chemical synthesis chemistry.chemical_compound Mice Structure-Activity Relationship In vivo Drug Discovery medicine Structure–activity relationship Animals Humans Molecular Biology Protein Kinase Inhibitors Cell Proliferation chemistry.chemical_classification biology Dose-Response Relationship Drug Molecular Structure Organic Chemistry Receptor Protein-Tyrosine Kinases Stereoisomerism Enzyme chemistry Enzyme inhibitor Drug Design biology.protein Molecular Medicine Drug Screening Assays Antitumor Tyrosine kinase
Zdroj:	Bioorganicmedicinal chemistry letters. 19(23)
ISSN:	1464-3405
Popis:	A series of N-(4-(6,7-disubstituted-quinolin-4-yloxy)-3-fluorophenyl)-2-oxo-3-phenylimidazolidine-1-carboxamides targeting c-Met and VEGFR2 tyrosine kinases was designed and synthesized. The compounds were potent against these two enzymes with IC(50) values in the low nanomolar range in vitro, possessed favorable pharmacokinetic profiles and showed high efficacy in vivo in several human tumor xenograft models in mice.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9a9020f89c6b464506c2acebb912014e https://pubmed.ncbi.nlm.nih.gov/19854051 Zobrazit plný text záznamu Full Text from ScienceDirect