Synthesis and Biological Evaluation of Novel Homopiperazine Derivatives as Anticancer Agents  

作　　者：Simin Teimoori Kuppusamy Panjamurthy Kambappa Vinaya Doddakunche S. Prasanna Sathees C. Raghavan Kanchugarakoppal S. Rangappa 

机构地区：[1]不详

出　　处：《Journal of Cancer Therapy》2011年第4期507-514,共8页癌症治疗（英文）

摘　　要：In search of new anticancer agents, a series of novel 1-benzhydryl-4-(substituted phenylcarboxamide / carbothioamide)-1,4-diazepane derivatives were designed, synthesized and characterized using 1H NMR, LCMS and elemental analysis. These molecules were evaluated for their anti-cancer activity by trypan blue exclusion and 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay on B-cell leukemic cell line, Reh. Carboxamide moiety containing derivatives showed good activity compared to the corresponding carbothioamide derivatives. In particular, 4-benzhydryl-N-(3-chlorophenyl)-1,4-diazepane-1-carboxamide showed good activity with IC50 value of 18 μM.In search of new anticancer agents, a series of novel 1-benzhydryl-4-(substituted phenylcarboxamide / carbothioamide)-1,4-diazepane derivatives were designed, synthesized and characterized using 1H NMR, LCMS and elemental analysis. These molecules were evaluated for their anti-cancer activity by trypan blue exclusion and 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay on B-cell leukemic cell line, Reh. Carboxamide moiety containing derivatives showed good activity compared to the corresponding carbothioamide derivatives. In particular, 4-benzhydryl-N-(3-chlorophenyl)-1,4-diazepane-1-carboxamide showed good activity with IC50 value of 18 μM.

关 键 词：CANCER THERAPY CYTOTOXICITY 1 4-Diazepane ISOCYANATES ISOTHIOCYANATES 

分 类 号：R73[医药卫生—肿瘤]