Design, synthesis and biological evaluation of naphthostyril derivatives as novel protein kinase FGFR1 inhibitors

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 µM. 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.

Drug design; FGFR1 inhibitor; naphthostyril; screening.