期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 23, 期 4, 页码 934-938出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2012.12.063
关键词
Indenoindolone; (Thio)semicarbazone; Oxime; Topoisomerase II; Anticancer agent
资金
- CSIR
- DBT
- ICMR, Government of India, New Delhi
Based on known heterocyclic topoisomerase II inhibitors and anticancer agents, various indenoindolone derivatives were predicted as potential topoisomerase II-inhibiting anticancer agents. They are hydrazones, (thio)semicarbazones, and oximes of indenoindolones, and indenoindolols. These derivatives with suitable substitutions exhibited potent specific inhibition of human DNA TopoII alpha, while not showing inhibition of topoisomerase I and DNA intercalation, despite the fact that parent indenoindolones are known poor/moderate inhibitors of topoisomerase II. The potent topoisomerase II inhibitor indenoindolone derivatives exhibited good anticancer activities compared to etoposide and 5-fluorouracil, and relatively low toxicity to normal cells. These derivatizations of indenoindolones were found to result in enhancement of anticancer activities. (C) 2012 Elsevier Ltd. All rights reserved.
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