Synthesis, Structural Characterization and Anticancer Activity of New 5-Trifluoromethyl-2-thioxo-thiazolo[4,5-]pyrimidine Derivatives.

Pharmaceuticals (Basel)

Department of Organic Chemistry and Pharmaceutical Technology, Faculty of Pharmacy, Wroclaw Medical University, 211A Borowska, 50-556 Wrocław, Poland.

Published: January 2022


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Article Abstract

Thiazolo[4,5-]pyrimidine derivatives are considered potential therapeutic agents, particularly in the development of anticancer drugs. In this study, new 7-oxo-(), 7-chloro-() and also three 7-amino-() 5-trifluoromethyl-2-thioxo-thiazolo[4,5-]pyrimidine derivatives have been synthesized and evaluated for their potential anticancer activity. These derivatives were characterized by spectroscopic methods and elemental analysis, and the single-crystal X-ray diffraction was further performed to confirm a 3D structure for compounds and . The antiproliferative activity evaluation of twelve new compounds was carried out on a variety of cell lines including four human cancer (A375, C32, DU145, MCF-7/WT) and two normal cell lines (CHO-K1 and HaCaT). Four of them (, , and ) were selected by the National Cancer Institute and evaluated for their in vitro anticancer activity using the NCI-60 screening program. 7-Chloro-3-phenyl-5-(trifluoromethyl)[1,3]thiazolo[4,5-]pyrimidine-2(3)-thione () proved to be the most active among the newly synthesized compounds.

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http://www.ncbi.nlm.nih.gov/pmc/articles/PMC8778818PMC
http://dx.doi.org/10.3390/ph15010092DOI Listing

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