Browsing by Author "Abuel-Maaty S.M."

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    Novel thienopyrimidine derivatives as dual EGFR and VEGFR-2 inhibitors: design, synthesis, anticancer activity and effect on cell cycle profile
    (Taylor and Francis Ltd, 2019) Mghwary A.E.-S.; Gedawy E.M.; Kamal A.M.; Abuel-Maaty S.M.; Department of Pharmaceutical Organic Chemistry; Faculty of Pharmacy; Cairo University; Cairo; Egypt; Department of Pharmaceutical Chemistry; Faculty of Pharmacy and Pharmaceutical Industries; Badr University in Cairo BUC; Cairo; Egypt; Department of Organic Chemistry; Faculty of Pharmacy; October University for Modern Science and Arts (MSA); Cairo; Egypt
    Aim: Design and synthesis of thienopyrimidine derivatives as dual EGFR and VEGFR-2 inhibitors.Material and methods: A series of novel 6,7,8,9-tetrahydro-5H-cyclohepta[4,5]thieno[2,3-d]pyrimidine derivatives with different substituents on C-4 position was synthesized and evaluated for their anticancer activity against MCF-7 cell line. EGFR, VEGFR-2 inhibitory assay, the cell cycle analysis and apoptosis induction ability of the most potent compound 5f were evaluated.Results: Most of the compounds showed moderate to significant anticancer activity. Compound 5f exhibited the most potent anticancer activity being 1.73- and 4.64-folds more potent than erlotinib and doxorubicin, respectively. Compound 5f showed potent EGFR inhibitory activity being 1.18-folds more potent than reference standard erlotinib and it also showed good VEGFR-2 inhibitory activity at the micromolar level with IC 50 value 1.23��M. Compound 5f caused induction of cell cycle arrest at G2/M phase and accumulation of cells in pre-G1 phase. Compound 5f induced cellular apoptosis. � 2019, � 2019 The Author(s). Published by Informa UK Limited, trading as Taylor & Francis Group.