Optimization of 7-alkene-3-quinolinecarbonitriles as Src kinase inhibitors

Autor:	Frank Boschelli, Judy Lucas, Daniel Wang, Erick Honores, Inder Chaudhary, Diane H. Boschelli, Jennifer M. Golas, Yan Wang, Biqi Wu, Ana Carolina Barrios Sosa
Rok vydání:	2010
Předmět:	Cellular activity Clinical Biochemistry Mice Nude Pharmaceutical Science Antineoplastic Agents Biochemistry Mice Microsomes Drug Discovery medicine Ic50 values Animals Humans Protein Kinase Inhibitors Molecular Biology Tumor xenograft chemistry.chemical_classification Kinase Alkene Organic Chemistry Xenograft Model Antitumor Assays src-Family Kinases Enzyme chemistry Quinolines Cancer research Molecular Medicine Bosutinib Proto-oncogene tyrosine-protein kinase Src medicine.drug
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 20:2924-2927
ISSN:	0960-894X
DOI:	10.1016/j.bmcl.2010.03.025
Popis:	The 7-alkene-3-quinolinecarbonitrile 20, a potent inhibitor of Src enzymatic and cellular activity with IC50 values of 2.1 and 58 nM, respectively, had comparable efficacy to bosutinib in a colon tumor xenograft study.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b1f894ee0202ec1e293be393b3575b38 https://doi.org/10.1016/j.bmcl.2010.03.025 Zobrazit plný text záznamu Full Text from ScienceDirect