Design, synthesis and biological evaluation of naphthostyril derivatives as novel protein kinase FGFR1 inhibitors
摘要:
New class of FGFR1 kinase inhibitors with naphthostyril heterocycle has been identified. A series of N-phenylnaphthostyril-1-sulfonamides has been synthesized and tested in vitro. It was revealed that the most active compound N-(4-hydroxyphenyl)naphthostyril-1-sulfonamide inhibited FGFR1 with IC50 of 2 mu M. In our preliminary studies, N-phenylnaphthostyril-1-sulfonamides demonstrated selectivity of FGFR1 inhibition and antiproliferative activity on cancer cell line. N-phenylnaphthostyril-1-sulfonamides have a good potential for further development as anticancer agents.
[EN] COMPOUNDS FOR USE IN THERAPY<br/>[FR] COMPOSÉS DESTINÉS À ÊTRE UTILISÉS EN THÉRAPIE
申请人:ACTAR AB
公开号:WO2009016081A2
公开(公告)日:2009-02-05
A compound of formula (I) wherein A is (C0-C1)-alkyl; R1 is (C1-C6)-alkyl when A is C1-alkyl and R1 is absent when A is C0-alkyl; R2 is optionally substituted mono- or polycyclic carbocyclyl or oxygen-containing heterocyclyl, R3 is H oroptionally substituted -S(O)2-NH-phenyl, and pharmaceutically acceptable salts thereof, for use as a medicament, e.g. in the treatment of inflammatory diseases and cancer.