Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 26, Issue 2, Pages 460-465Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2015.11.092
Keywords
Hexahydropyrrolo[2,3-b]indole; Imidazolium salts; Structure-activity relationships
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Funding
- Program for Changjiang Scholars and Innovative Research Team in University [IRT13095]
- Natural Science Foundation of China [21462049, 21332007, U1402227]
- Natural Science Foundation of Yunnan Province [2013FA028, 2012FB113]
- Education Department of Yunnan Province [ZD2014010]
- Program for China Scholarship Council [201408535034]
- excellent young talents of Yunnan University
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A series of novel hexahydropyrrolo[2,3-b]indole-1H-imidazolium salts were synthesized and evaluated in vitro against a panel of human tumor cell lines. The results suggest that the 5,6-dimethyl-benzimidazole ring, and substitution of the imidazolyl-3-position with a 2-bromobenzyl or 2-naphthylmethyl group, were important for the cytotoxic activity. Notably, Compound 43, bearing a 2-bromobenzyl substituent at position-3 of 5,6-dimethyl-benzimidazole, was found to possess the most potent derivative against five human tumor cell lines with IC50 values below 2.68 mu M and more selective towards SMMC-7721, A549 and SW480 cell lines. Compounds 25 and 39 were more selective to HL-60 and MCF-7 cell lines with IC50 values of 0.47 and 1.46 mu M. (C) 2015 Published by Elsevier Ltd.
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