logo
English (United Kingdom)Ukrainian (UA)
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.

Other kinase inhibitors research:

ASK1 Inhibitors
Evaluation of 2-Thioxo-thiazolidin-4-ones Derivatives as Inhibitors of ASK1 Image
In order to discover novel ASK1 inhibitors we have performed screening program,...



 

FGFR1 Inhibitors
Quinazolines Image
Quinazolines is another known class of RTK inhibitors that is widely...



 

CK2 Inhibitors
3-hydroxy-4'-carboxyflavone derivatives (FLC) Image
With the aim to identify new CK2 inhibitors virtual screening of 150,000 small...



 

© 2012 All rights reserved
footer logo