

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

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.
Latvian Institute of Organic Synthesis - Aizkraukles iela, 21, Riga, LV-1006, Latvia - hgs@osi.lv