title: Design, synthesis and biological evaluation of naphthostyril derivatives as novel protein kinase FGFR1 inhibitors.
abstract: 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.
authors.affiliation: Medicinal Chemistry Department and.
authors.forename: Andrii Anatoliyovych
authors.initials: AA
authors.lastname: Gryshchenko
authors.forename: Kostiantyn Vasyliovych
authors.initials: KV
authors.lastname: Levchenko
authors.forename: Volodymyr Grygorovich
authors.initials: VG
authors.lastname: Bdzhola
authors.forename: Tatiana Panasivna
authors.initials: TP
authors.lastname: Ruban
authors.forename: Lyubov Leonidovna
authors.initials: LL
authors.lastname: Lukash
authors.forename: Sergiy Mikolayovych
authors.initials: SM
authors.lastname: Yarmoluk
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D015870:Gene Expression; D006801:Humans; D020128:Inhibitory Concentration 50; D011804:Quinolines / Q000138:chemical synthesis* / Q000494:pharmacology; D051496:Receptor, Fibroblast Growth Factor, Type 1 / Q000037:antagonists & inhibitors* / Q000235:genetics; D013343:Styrenes / Q000138:chemical synthesis* / Q000494:pharmacology; D013449:Sulfonamides / Q000138:chemical synthesis* / Q000494:pharmacology
chemical_list: D000970:Antineoplastic Agents; D011804:Quinolines; D013343:Styrenes; D013449:Sulfonamides; C496348:FGFR1 protein, human; D051496:Receptor, Fibroblast Growth Factor, Type 1
keywords: Drug design; FGFR1 inhibitor; naphthostyril; screening