Author(s)

Simin Teimoori, Kuppusamy Panjamurthy, Kambappa Vinaya, Doddakunche S. Prasanna, Sathees C. Raghavan, Kanchugarakoppal S. Rangappa

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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.

Cancer Therapy, Cytotoxicity, 1, 4-Diazepane, Isocyanates, Isothiocyanates

S. Teimoori, K. Panjamurthy, K. Vinaya, D. Prasanna, S. Raghavan and K. Rangappa, "Synthesis and Biological Evaluation of Novel Homopiperazine Derivatives as Anticancer Agents," Journal of Cancer Therapy, Vol. 2 No. 4, 2011, pp. 507-514. doi: 10.4236/jct.2011.24069.