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.
Highlights
Cancer remains the leading cause of death in the World and as a result there is a pressing need for novel and effective treatments
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
Summary
Cancer remains the leading cause of death in the World and as a result there is a pressing need for novel and effective treatments. Combined anticancer therapies or multi-acting drugs are clinically preferred to traditional cytotoxic treatment, with the aim of overcoming resistance and toxicity drawbacks. These events often prevent successful treatment and are responsible for reduced survival times [3,4]. In the past 50 years, the mass screening of either synthetic derivatives or natural products has led to the discovery of the currently utilized anticancer drugs. Homopiperazine or 1,4-diazepane ring system has demonstrated considerable utility in drug design, with derivatives demonstrating a wide range of biological activities. In continuation of our efforts to get new chemotherapeutic agents [16,17,18], we report the synthesis of homopiperazine derivatives and their antiproliferative activity
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