Article
Design, synthesis, docking, MD simulations, and anti-proliferative evaluation of thieno[2,3-d]pyrimidine derivatives as new EGFR inhibitors.
Journal of enzyme inhibition and medicinal chemistry - 1 Dec 2023
Sobh Eman A, Dahab Mohammed A, Elkaeed Eslam B, Alsfouk Aisha A, Ibrahim Ibrahim M, Metwaly Ahmed M, Eissa Ibrahim H
Abstract excerpt
A group of EGFR inhibitors derived from thieno[2,3-d]pyrimidine nucleus was designed, synthesised, and examined as anti-proliferative lead compounds. MCF-7 and A549 cell lines were inhibited by 5b, the most active member. It had inhibitory partialities of 37.19 and 204.10 nM against EGFRWT and EGFRT790M, respectively. Compound 5b was 2.5 times safer against the WI-38 normal cell lines than erlotinib. Also, it...
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