On January 31, 2020, Alkahtani, Hamad M.; Abdalla, Ashraf N.; Obaidullah, Ahmad J.; Alanazi, Mohammed M.; Almehizia, Abdulrahman A.; Alanazi, Mashael G.; Ahmed, Ahmed Y.; Alwassil, Osama I.; Darwish, Hany W.; Abdel-Aziz, Alaa A.-M.; El-Azab, Adel S. published an article.COA of Formula: C2H4ClNO The title of the article was Synthesis, cytotoxic evaluation, and molecular docking studies of novel quinazoline derivatives with benzenesulfonamide and anilide tails: Dual inhibitors of EGFR/HER2. And the article contained the following:
We synthesized a new series of 2-[(3-(4-sulfamoylphenethyl)-4(3H)-quinazolinon-2-yl)thio]anilide derivatives (2-16) and evaluated their cytotoxic activity against breast adenocarcinoma (MCF-7), colorectal adenocarcinoma (HT-29), and acute myeloid leukemia (HL-60 and K562) cells. To reveal their selectivity toward cancer cells, the compounds were also tested against the human fibroblast cell line, MRC-5. Compounds 1-5 exhibited potent cytotoxic activity against the tested cell lines with IC50 values of 0.65-3.86, 0.68-4.60, 0.41-1.45, 0.42-4.07, and 3.77-25.55μM, resp. compared to sorafenib, the standard drug (IC50 2.50, 2.50, and 3.14μM against MCF-7, HT-29, and HL60 cells, resp.). Interestingly, compounds 1-5 displayed selectivity toward the cancer cell lines over MRC-5 (IC50 3.77-25.55μM). These compounds also displayed potent inhibitory activity against EGFR and HER2 kinases (IC50 0.09-0.43 and 0.15-0.33μM, resp.) compared to the standard drug, sorafenib (IC50 0.11 and 0.13μM, resp.). Likewise, compounds 1, 4, and 5 showed strong inhibitory activity against VEGFR2 (IC50 0.34, 0.28 and 0.39μM, resp.) compared to sorafenib (IC50 0.17μM). We also employed mol. docking to identify the structural features required for the EGFR/HER2 inhibitory activity of the new series. Ultimately, compounds 1, 4, and 5 were demonstrated to be candidates for further preclin. investigations. The experimental process involved the reaction of 2-Chloroacetamide(cas: 79-07-2).COA of Formula: C2H4ClNO
The Article related to preparation quinazoline benzenesulfonamide anilide derivative egfr her2 inhibitor cancer, anticancer, egfr, her2, molecular docking, quinazolin-4-ones, Pharmacology: Structure-Activity and other aspects.COA of Formula: C2H4ClNO
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