Synthesis and biological evaluation of novel thiazolo[4,5-d]pyrimidin-7(6H)-ones as topoisomerase I inhibitors,Chemistry of Heterocyclic Compounds

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Synthesis and biological evaluation of novel thiazolo[4,5-d]pyrimidin-7(6H)-ones as topoisomerase I inhibitors
Chemistry of Heterocyclic Compounds ( IF 1.4 ) Pub Date : 2022-01-27 , DOI: 10.1007/s10593-021-03046-7
Laichun Luo ₁ , Qiang Wang ₁ , Yuanhang Xiang ₁ , Xiaozhi Peng ₁ , Chunling Hu ₁

Affiliation

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.

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