Search for FGFR1 inhibitors among oxindole derivatives.

Authors :: Gryshchenko, A. A.
Bdzhola, V. G.
Borovikov, O. V.
Kukharenko, O. P.
Pletnyova, L. V.
Yarmoluk, S. M.
Source :: Ukrainica Bioorganica Acta. 2009, Vol. 7 Issue 2, p64-68. 5p. 1 Diagram, 1 Chart.
Publication Year :: 2009
Abstract: Protein kinase FGFR1 plays a key role in oncogenic transformation and oncovasculogenesis. Inhibitors of this kinase can be used as anticancer drugs. Protein kinase FGFR1 inhibitors searching were performed among oxindole derivatives. 9 compounds from 920 oxindole derivatives have been chosen using virtual screening. The most active compound was 2-Hydroxybenzoic acid (2-oxo-1,2-dihydroindol-3-ylidene)-hydrazide (??50 1.25 μM). Structure-activity relationship of tested compounds was investigated and optimization strategies were proposed. [ABSTRACT FROM AUTHOR]