Evolution of a New Class of VEGFR-2 Inhibitors from Scaffold Morphing and Redesign.

ABSTRACT: Anti-VEGF therapy is a clinically validated treatment for age-related macular degeneration (AMD). We have recently reported the discovery of oral VEGFR-2 inhibitors that are selectively distributed to the ocular tissues. Herein we report a further development of those compounds and in particular the validation of the hypothesis that aminoheterocycles such as aminoisoxazoles and aminopyrazoles could also function as effective "hinge" binding moieties leading to a new class of KDR (kinase insert domain containing receptor) inhibitors.

SUBMITTER: Mainolfi N 

PROVIDER: S-EPMC4834667 | biostudies-literature | 2016 Apr

REPOSITORIES: biostudies-literature