Design, synthesis and biological evaluation of some furan and furopyrimidine derivatives as novel anti-cancer agents / Manar Abdelkarim Kassem Ezz Eldin ; Supervised Safinaz Elsayed Abbas Ibrahim , Essam Eldin A. Osman , Akram Hifny Abdelhaleem

Thesis (M.Sc.) - Cairo University - Faculty of Pharmacy - Department of Pharmaceutical Chemistry

Cancer causes the rapid uncontrolled growth of abnormal cells forming a solid mass tumor or neoplasmwhich proliferates to new sites in the body causing additional tumors by a process called metastasis, patients die from metastatic spread to vital organs rather than from their primary tumors. Many types of cancer treatment are available, but there wasn't any cancer treatment can cure, shrink or stop the progression without affecting the healthy cells, so there always need for targeted cancer therapy with more precision and potentially fewer side effects.Many furans and furopyrimidine derivatives are well known to have significant anti-cancer activity through various mechanisms of action.Thus, in this study, new furan derivatives namely: 4,5-diphenyl-2-((4-(substituted) benzylidene) amino) furan-3-carbonitrile (IVa-c) and their reduced form (Va-c), 2- [(4-hydroxy-3-methoxy-5-(substitutedmethyl)benzylidene)amino]-4,5-diphenylfuran-3-carbonitrile (VIIa-d) and their reduced form(VIIIa-d), iminomethylacid hydrazide derivatives(XIIIa,b), furopyrimidines(XIb, XIVa-d) and furotriazolopyrimidines(XIa, XVa-d)were designed, synthesized and evaluated for their invitro anticancer activity at NCI, USA.The most active furan derivative VIIIcwhich exhibited a significant growth inhibition% against twenty-one cell lines ranging from 174.62-50.17% was further subjected to IC50 calculations, cellcycle analysis and apoptosis assay, in addition to enzyme inhibition assay againstBRAF and CDK2A enzymes

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