Synthesis, characterization, and in vitro anticancer evaluation of 2,4 disulfonylsubstituted 5-aminothiazoles

Zyabrev, V.; Demydchuk, B.; Pilyo, S.; Zhirnov, V.; Liavynets, O.; Brovarets, V.

Growing Science » Current Chemistry Letters » Synthesis, characterization, and in vitro anticancer evaluation of 2,4 disulfonylsubstituted 5-aminothiazoles

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Current Chemistry Letters

ISSN 1927-730x (Online) - ISSN 1927-7296 (Print) Quarterly Publication Volume 13 Issue 3 pp. 557-568 , 2024

Synthesis, characterization, and in vitro anticancer evaluation of 2,4 disulfonylsubstituted 5-aminothiazoles Pages 557-568 Download PDF

Authors: Volodymyr Zyabrev, Bohdan Demydchuk, Stepan Pilyo, Victor Zhirnov, Olexandr Liavynets, Volodymyr Brovarets

DOI: 10.5267/j.ccl.2024.2.003

Keywords: 4-Arylsulfonyl-1, 3-thiazoles, Design, Synthesis, Anticancer activity, COMPARE correlations

Abstract: Novel 2,4-disulfonylsubstituted 5-aminothiazoles were synthesized and their anticancer activity was assessed at a high dose (10 μM) against NCI 60 cancer cell lines. Compounds 24 and 25 showed the antiproliferative activity with mean growth inhibition about 66.0%. Replacing 4-hydroxypiperidine 24 with the more hydrophilic N-methyl piperazine 25 increased the number of sensitive cell lines while replacing these hydrophilic groups with lipophilic ones abolished the anticancer activity. The COMPARE analysis showed that the tested compounds had a moderate positive correlation with alkylating agents (CCNU and methyl CCNU) and with a purine nucleotide biosynthesis inhibitor analog (L-cysteine). The results indicate that the above mechanisms of antitumor action of standard compounds are not the main ones for the tested compounds due to the lack of a high correlation. The results of this study allow us to consider compounds 24 and 25 as a basis for their further functionalization to obtain more active compounds.

How to cite this paper

 Zyabrev, V., Demydchuk, B., Pilyo, S., Zhirnov, V., Liavynets, O & Brovarets, V. (2024). Synthesis, characterization, and in vitro anticancer evaluation of 2,4 disulfonylsubstituted 5-aminothiazoles.Current Chemistry Letters, 13(3), 557-568.

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