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

Authors

  • Laichun Luo Key Laboratory of Chinese Medicine Chemistry and Chinese Herbal Compound of Hubei Province, Hubei University of Chinese Medicine, Wuhan 430065, China
  • Qiang Wang Key Laboratory of Chinese Medicine Chemistry and Chinese Herbal Compound of Hubei Province, Hubei University of Chinese Medicine, Wuhan 430065, China
  • Yuanhang Xiang Key Laboratory of Chinese Medicine Chemistry and Chinese Herbal Compound of Hubei Province, Hubei University of Chinese Medicine, Wuhan 430065, China
  • Xiaozhi Peng Key Laboratory of Chinese Medicine Chemistry and Chinese Herbal Compound of Hubei Province, Hubei University of Chinese Medicine, Wuhan 430065, China
  • Chunling Hu Key Laboratory of Chinese Medicine Chemistry and Chinese Herbal Compound of Hubei Province, Hubei University of Chinese Medicine, Wuhan 430065, China

DOI:

https://doi.org/10.1007/6419

Keywords:

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

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.

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Published

2021-12-15

Issue

Vol. 57 No. 12 (2021)

Section

Original Papers