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Bioorg Med Chem. 2008 Apr 15;16(8):4617-25. doi: 10.1016/j.bmc.2008.02.036. Epub 2008 Feb 15.

Synthesis, cytotoxic activities and structure-activity relationships of topoisomerase I inhibitors: indolizinoquinoline-5,12-dione derivatives.

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1
School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510080, China.

Abstract

A series of indolizinoquinoline-5,12-dione derivatives (IQDs) are synthesized and evaluated for their cytotoxic activities toward human lung adenocarcinoma (GLC-82), large-cell lung carcinoma (NCI-H460), promyelocytic leukemia (HL-60) and breast carcinoma (MCF-7) cells by MTT method. Most of the IQDs show significant cytotoxic potency. In addition, the evaluation of structure-activity relationships indicated that the incorporation of electron-withdrawing substituents at the C or D ring will enhance the activities of the target compounds distinctly. The topoisomerase I inhibitory activity is also measured.

PMID:
18296054
DOI:
10.1016/j.bmc.2008.02.036
[Indexed for MEDLINE]

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