127007-22-1Relevant academic research and scientific papers
Design, synthesis and biological evaluation of benzimidazole-rhodanine conjugates as potent topoisomerase II inhibitors
Li, Penghui,Zhang, Wenjin,Jiang, Hong,Li, Yongliang,Dong, Changzhi,Chen, Huixiong,Zhang, Kun,Du, Zhiyun
, p. 1194 - 1205 (2018)
In this study, a series of benzimidazole-rhodanine conjugates were designed, synthesized and investigated for their topoisomerase II (Topo II) inhibitory and cytotoxic activities. The results from Topo II-mediated pBR322 DNA relaxation and cleavage assays showed that the synthesized compounds might act as Topo II catalytic inhibitors. Certain compounds displayed potent Topo II inhibition at 10 μM. The cytotoxic activities of these compounds against HeLa, A549, Raji, PC-3, MDA-MB-201, and HL-60 cancer cell lines were evaluated. The results indicated that these compounds exhibited strong antiproliferative activity. A good relationship was observed between the Topo II inhibitory potency and the cytotoxicity of these compounds. The structure-activity relationship revealed that the electronic effects, the phenyl group, and the rhodanine moiety were particularly important for the Topo II inhibitory potency and cytotoxicity.
Synthesis, structure and reactivity of 1-(4-nitrobenzyl)-2-chloromethyl benzimidazole
Sparke, Amanda E.,Fisher, Christopher M.,Mewis, Ryan E.,Archibald, Stephen J.
body text, p. 4723 - 4726 (2010/09/20)
The synthesis of 1-(4-nitrobenzyl)-2-chloromethyl benzimidazole, which undergoes a nucleophilic substitution with pyridine in the absence of additional base, is reported. The key steps are the reaction of 1,2-phenylenediamine to give exclusively the mono-
Angiotensin II receptor blocking benzimidazoles
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, (2008/06/13)
Substituted benzimidazoles such as STR1 and pharmaceutically suitable salts thereof are useful as angiotensin II blockers. These compounds have activity in treating hypertension and congestive heart failure.
