Browsing by Author "Kamal A.M."

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    Design, synthesis and cytotoxic activity of certain novel chalcone analogous compounds
    (Elsevier Masson SAS, 2017) El-Meligie S.; Taher A.T.; Kamal A.M.; Youssef A.; Pharmaceutical Organic Chemistry Department; Faculty of Pharmacy; Cairo University; Cairo; 11561; Egypt; Pharmaceutical Organic Chemistry Department; Faculty of Pharmacy; October University for Modern Sciences and Arts (MSA); Giza; Egypt; Pharmaceutical Organic Chemistry Department; Faculty of Pharmacy and Drug Manufacturing; Misr University for Science and Technology; Giza; Egypt
    A series of chalcone analogous compounds were designed and synthesized. Replacing/substituting the enone or ethylenic bridge of the parent chalcone with rigid heterocyclic moieties or substituted aromatic amines gave nineteen target compounds. Their cytotoxic activities were screened against both breast and liver cancer cells as well as breast and liver normal cells. Target compounds were also evaluated for their inhibition activity of tubulin beta polymerization. Target compound 2e, 3a, 3b, 3c, 4a-4d, 5a, 5b and 6 showed broad spectrum excellent anticancer activity against both MCF-7 and HepG2. Compound 4a showed the most TUBb inhibition activity. � 2016 Elsevier Masson SAS
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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.
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    Synthesis, characterisation and biological screening of some 2-substituted benzimidazole derivatives as potential anticancer agents
    (Science Reviews 2000 Ltd, 2016) Shaaban M.A.-E.; Kamal A.M.; Teba H.E.-S.; Pharmaceutical Organic Chemistry Department; Faculty of Pharmacy; Cairo University; Cairo; 11561; Egypt; Pharmaceutical Organic Chemistry Department; Faculty of Pharmacy; October University for Modern Sciences and Arts (MSA); Cairo; Egypt
    Twenty two new polycyclic compounds containing a 2-substituted benzimidazole core were synthesised, characterised and evaluated in vitro against the three most widespread cancers. Seven compounds showed outstanding antitumor activity towards breast, lung or central nervous system cancer cell lines.