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RESEARCH Protein Kinase Inhibitors FGFR1 Inhibitors N-phenylnaphthostyril-1-sulfonamides

N-phenylnaphthostyril-1-sulfonamides

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.

fgfr1_im4_new1
Figure 1. N-phenylnaphthostyril-1-sulfonamide inhibitor of FGFR1.


  • A.A. Gryshchenko, K.V. Levchenko, V.G. Bdzhola, T.P. Ruban, L.L. Lukash, S.M. Yarmoluk. (2015) Design, synthesis and biological evaluation of naphthostyril derivatives as novel protein kinase FGFR1 inhibitors. J Enzyme Inhib Med Chem 30(1):126-132.

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