Synthesis, biological evaluations and molecular modelling studies of novel indolin-2-ones designing as FGFR inhibitors.

ABSTRACT: A series of novel 3,5-disubstituted indolin-2-ones were designed and synthesized as selective FGFR inhibitors. In the design process of 3,5-disubstituted indolin-2-ones for FGFRs, molecular docking studies were performed to generate and optimize novel compounds which have FGFR inhibitory potency, theoretically. In vitro enzyme inhibitory and selectivity profiles of the synthesized compounds, and their cytotoxicity against NIH-3T3 cells were evaluated. According to enzyme inhibition assay, compound A1 (FGFR1-4; IC₅₀ = 19.82; 5.95; 1419; 37150 nM), compound A5 (FGFR1-4; IC₅₀ = 1890; Nd; 6.50; 18590 nM) and compound A13 (FGFR1-4; IC₅₀ = 6.99; 1022; 17090; 8993 nM) have displayed best inhibitory potency against FGFR2, FGFR3 an

SUBMITTER: Coban G 

PROVIDER: S-EPMC6978637 | biostudies-literature | 2019 Nov

REPOSITORIES: biostudies-literature