On August 31, 2022, Sobh, Eman A.; Khalil, Nadia A.; Faggal, Samar I.; Hassan, Marwa S. A. published an article.Application of 79-07-2 The title of the article was New benzothienopyrimidine derivatives as dual EGFR/ARO inhibitors: Design, synthesis, and their cytotoxic effect on MCF-7 breast cancer cell line. And the article contained the following:
New cytotoxic agents based on benzothienopyrimidine scaffold were designed, synthesized, and evaluated against the MCF-7 breast cancer line in comparison to erlotinib and letrozole as reference drugs. Eight compounds demonstrated up to 20-fold higher anticancer activity than erlotinib, and five of these compounds were up to 11-fold more potent than letrozole in MTT assay. The most promising compounds were evaluated for their inhibitory activity against EGFR and ARO enzymes. Compound 12, which demonstrated potent dual EGFR and ARO inhibitory activity with IC50 of 0.045 and 0.146 μM, resp., was further evaluated for caspase-9 activation, cell cycle anal., and apoptosis. The results revealed that the tested compound 12 remarkably induced caspase-9 activation (IC50 = 16.29 ng/mL) caused cell cycle arrest at the pre-G1/G1 phase and significantly increased the concentration of cells at both early and late stage of apoptosis. In addition, it showed a higher safety profile on normal MCF-10A cells, and higher antiproliferative activity on cancer cells (IC50 = 8.15 μM) in comparison to normal cells (IC50 = 41.20 μM). It also revealed a fivefold higher selectivity index than erlotinib towards MCF-7 cancer cells. Docking studies were performed to rationalize the dual inhibitory activity of compound 12. The experimental process involved the reaction of 2-Chloroacetamide(cas: 79-07-2).Application of 79-07-2
The Article related to benzothienopyrimidine derivative preparation aromatase egfr inhibitor antitumor activity, aro and egfr inhibitors, benzothienopyrimidine, cytotoxic, Placeholder for records without volume info and other aspects.Application of 79-07-2
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