Article
Design, synthesis, and anti-cancer evaluation of new pyrido[2,3-d]pyrimidin-4(3H)-one derivatives as potential EGFRWT and EGFRT790M inhibitors and apoptosis inducers.
Journal of enzyme inhibition and medicinal chemistry - 1 Dec 2022
Elzahabi Heba S A, Nossier Eman S, Alasfoury Rania A, El-Manawaty May, Sayed Sara M, Elkaeed Eslam B, Metwaly Ahmed M, Hagras Mohamed, Eissa Ibrahim H
Abstract excerpt
A new series of pyrido[2,3-d]pyrimidin-4(3H)-one derivatives having the essential pharmacophoric features of EGFR inhibitors has been designed and synthesised. Cell viability screening was performed for these compounds against A-549, PC-3, HCT-116, and MCF-7 cell lines at a dose of 100 μM. The highest active derivatives (8a, 8 b, 8d, 9a, and 12b) were selected for IC50 screening. Compounds 8a, 8 b, and 9a showed...
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