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

Mainolfi, Nello and Karki, Rajeshri and Liu, Fang and Anderson, Karen (2016) Evolution of a New Class of VEGFR-2 Inhibitors from Scaffold Morphing and Redesign. ACS Med Chem Letters, 7 (4). pp. 363-367. ISSN 1948-58751948-5875

Abstract

Anti VEGF therapy has been a clinically validated treatment for age related macular degeneration (AMD). We have recently reported the discovery of indole carboxamide based oral VEGFR-2 inhibitors bearing a bicyclic pyrimidine as “hinge” binding motif and an aminoheterocycle occupying the back-pocket of the kinase catalytic site. Herein we report a further development of this series of compounds and in particular the validation of the hypothesis that aminoheterocycles such as aminoisoxazoles and aminopyrazoles (present in the urea) could also function as effective “hinge” binding moieties leading to a new class of KDR (Kinase Insert Domain containing receptor) inhibitors.

Item Type: Article
Date Deposited: 18 Apr 2016 23:45
Last Modified: 18 Apr 2016 23:45
URI: https://oak.novartis.com/id/eprint/24591

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