TITLE:
Synthesis and Biological Evaluation of Novel Homopiperazine Derivatives as Anticancer Agents
AUTHORS:
Simin Teimoori, Kuppusamy Panjamurthy, Kambappa Vinaya, Doddakunche S. Prasanna, Sathees C. Raghavan, Kanchugarakoppal S. Rangappa
KEYWORDS:
Cancer Therapy, Cytotoxicity, 1, 4-Diazepane, Isocyanates, Isothiocyanates
JOURNAL NAME:
Journal of Cancer Therapy,
Vol.2 No.4,
October
12,
2011
ABSTRACT: 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.