Synthesis, cytotoxic activities and structure-activity relationships of topoisomerase I inhibitors: indolizinoquinoline-5,12-dione derivatives |
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Authors: | Cheng Yu An Lin-Kun Wu Ning Wang Xiao-Dong Bu Xian-Zhang Huang Zhi-Shu Gu Lian-Quan |
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Affiliation: | School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510080, China. |
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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. |
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