New Benzimidazole-, 1,2,4-Triazole-, and 1,3,5-Triazine-Based Derivatives as Potential EGFRWT and EGFRT790M Inhibitors: Microwave-Assisted Synthesis, Anticancer Evaluation, and Molecular Docking Study
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DOI: 10.1021/acsomega.1c06836
Abstract: A new series of benzimidazole, 1,2,4-triazole, and 1,3,5-triazine derivatives were designed and synthesized using a microwave irradiation synthetic approach utilizing 2-phenylacetyl isothiocyanate (1) as a key starting material. All the new analogues were evaluated as… read more here.
Keywords: egfrwt egfrt790m; benzimidazole triazole; triazole triazine; egfrt790m inhibitors ... See more keywords
Design, synthesis, and molecular docking studies of novel pomalidomide-based PROTACs as potential anti-cancer agents targeting EGFRWT and EGFRT790M
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DOI: 10.1080/14756366.2022.2062338
Abstract: Abstract A new class of EGFR PROTACs based on pomalidomide was developed, synthesised, and tested for their cytotoxic activity against a panel of human cancer cells. Compounds 15–21 were showed to be more effective against… read more here.
Keywords: molecular docking; design synthesis; egfrwt egfrt790m; synthesis molecular ... See more keywords
Discovery of new 1H-pyrazolo[3,4-d]pyrimidine derivatives as anticancer agents targeting EGFRWT and EGFRT790M
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DOI: 10.1080/14756366.2022.2112575
Abstract: Abstract New 1H-pyrazolo[3,4-d]pyrimidine derivatives were designed and synthesised to act as epidermal growth factor receptor inhibitors (EGFRIs). The synthesised derivatives were assessed for their in vitro anti-proliferative activities against A549 and HCT-116 cancer cells. Compounds… read more here.
Keywords: new pyrazolo; egfrwt egfrt790m; pyrazolo pyrimidine; compound 12b ... See more keywords
Design, synthesis, apoptotic, and antiproliferative effects of 5-chloro-3- (2-methoxyvinyl)-indole-2-carboxamides and pyrido[3,4-b]indol-1-ones as potent EGFRWT/EGFRT790M inhibitors
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DOI: 10.1080/14756366.2023.2218602
Abstract: Abstract A new series of indole-2-carboxamides 5a-g, 6a-f and pyrido[3,4-b]indol-1-ones 7a and 7b have been developed as new antiproliferative agents that target both wild and mutant type EGFR. The antiproliferative effect of the new compounds… read more here.
Keywords: design synthesis; egfrwt egfrt790m; indole carboxamides; carboxamides pyrido ... See more keywords