Title : Scaffold hopping and redesign approaches for quinazoline based urea derivatives as potent VEGFR-2 inhibitors.

Pub. Date : 2020 Aug

PMID : 32480170






2 Functional Relationships(s)
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1 Five quinazoline -2-carboxamide derivatives (5d, 5e, 5 h, 5i, 5j) revealed potent nanomolar VEGFR-2 inhibition with IC50 values of 12.1, 40.3, 15.5, 13.1 and 57.4 nM, respectively, superior to that of the reference drug sorafenib (IC50 78.9 nM). Sorafenib kinase insert domain receptor Homo sapiens
2 Furthermore, molecular modeling study was administered to realize any clarification of the binding mode in the inactive VEGFR-2 conformation that demonstrates compatible binding modes similar to those of sorafenib and regorafenib. Sorafenib kinase insert domain receptor Homo sapiens