Synthesis and structure–activity relationships of novel benzofuran farnesyltransferase inhibitors

Autor:	Yasuhiko Shiratori, Hirosato Ebiike, Takaaki A. Fukami, Masahiro Sakaitani, Toshiyuki Tsukaguchi, Yuko Aoki, Nobuya Ishii, Kohsuke Asoh, Kenichi Kawasaki, Tatsuo Ohtsuka, Miyako Masubuchi, Nobuo Shimma, Osamu Kondoh, Ikumi Hyoudoh, Masami Kohchi
Rok vydání:	2009
Předmět:	Chemistry Pharmaceutical Farnesyltransferase Clinical Biochemistry Pharmaceutical Science Antineoplastic Agents Quinolones Crystallography X-Ray Biochemistry Chemical synthesis Inhibitory Concentration 50 Mice Structure-Activity Relationship chemistry.chemical_compound In vivo Drug Discovery medicine Animals Farnesyltranstransferase Humans Enzyme Inhibitors Benzofuran Molecular Biology Benzofurans chemistry.chemical_classification Farnesyl-diphosphate farnesyltransferase biology Chemistry Organic Chemistry In vitro Enzyme Drug Design biology.protein Molecular Medicine Tipifarnib Drug Screening Assays Antitumor Neoplasm Transplantation medicine.drug
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 19:1753-1757
ISSN:	0960-894X
DOI:	10.1016/j.bmcl.2009.01.074
Popis:	A series of benzofuran-based farnesyltransferase inhibitors have been designed and synthesized as antitumor agents. Among them, 11f showed the most potent enzyme inhibitory activity (IC 50 = 1.1 nM) and antitumor activity in human cancer xenografts in mice.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::05fa59cee8e2a785c9bbfd09094f894f https://doi.org/10.1016/j.bmcl.2009.01.074 Zobrazit plný text záznamu Full Text from ScienceDirect