European Journal of Medicinal Chemistry
European Journal of Medicinal Chemistry
5 years ago

Novel methyl indolinone-6-carboxylates containing an indole moiety as angiokinase inhibitors

Novel methyl indolinone-6-carboxylates containing an indole moiety as angiokinase inhibitors
A novel series of methyl indolinone-6-carboxylates bearing an indole moiety were identified as potent angiokinase inhibitors. The most active compound, A8, potently targeted the kinase activities of vascular endothelial growth factor receptors 2 and 3, and platelet-derived growth factor receptors α and β, with IC50 values in the nanomolar range. In addition, A8 effectively suppressed the proliferation of human umbilical vein endothelial cells, and HT-29 and MCF-7 cancer cells, by inducing apoptosis. Compound A8 is thus a promising candidate for further investigation.

Publisher URL: www.sciencedirect.com/science

DOI: S0223523417306347

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