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SYNTHESIS AND BIOLOGICAL EVALUATION OF NOVEL THIAZOLO[4,5-d]PYRIMIDIN-7(6H)-ONES AS TOPOISOMERASE I INHIBITORS

Laichun Luo, Qiang Wang, Yuanhang Xiang, Xiaozhi Peng, Chunling Hu
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Abstract


A series of novel thiazolo[4,5-d]pyrimidin-7(6H)-ones were designed, synthesized, and evaluated as anticancer agents. Among them, two compounds demonstrated potent cytotoxicity and topoisomerase I inhibitory activity. In addition, their possible binding modes with topoisomerase I/DNA complex were proposed on the basis of molecular docking results.


Keywords


iodine; thiazolo[4,5-d]pyrimidin-7(6H)-one; topoisomerase I; anticancer activity; molecular docking.

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