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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.



中文翻译:

新型噻唑并[4,5-d]嘧啶-7(6H)-ones作为拓扑异构酶I抑制剂的合成及生物学评价

设计、合成了一系列新型噻唑并[4,5 - d ]嘧啶-7(6 H )-酮作为抗癌剂。其中,两种化合物表现出强大的细胞毒性和拓扑异构酶 I 抑制活性。此外,在分子对接结果的基础上,提出了它们与拓扑异构酶I/DNA复合物可能的结合方式。

更新日期:2022-01-27
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