Дизайн, синтез і біологічне дослідження похідних нафтостирилу як нових інгібіторів протеїнкінази FGFR1

Наша стаття про розробку нових інгібіторів протеїнкінази FGFR1 була опублікована в журналі Journal of Enzyme Inhibition and Medicinal Chemistry

Тези: 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.

• Design, synthesis and biological evaluation of naphthostyril derivatives as novel protein kinase FGFR1 inhibitors Gryshchenko AA, Levchenko KV, Bdzhola VG, Ruban TP, Lukash LL, Yarmoluk SM. J Enzyme Inhib Med Chem. 2014, DOI: 10.3109/14756366.2014.895718.