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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

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

Mainolfi Nello N Karki Rajeshri R Liu Fang F Anderson Karen K

ACS medicinal chemistry letters 20160202 4

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 d ...[more]

PMID: 27096042

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