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Sci. Pharm. 2018, 86(4), 47; https://doi.org/10.3390/scipharm86040047

Isothiochromenothiazoles—A Class of Fused Thiazolidinone Derivatives with Established Anticancer Activity That Inhibits Growth of Trypanosoma brucei brucei

1
Department of Pharmaceutical, Organic and Bioorganic Chemistry, Danylo Halytsky Lviv National Medical University, Pekarska 69, 79010 Lviv-10, Ukraine
2
UMR 7245 CNRS MCAM, Muséum National d’Histoire Naturelle, Sorbonne Universités, CP 52, 57 rue Cuvier, Paris 75005, France
*
Author to whom correspondence should be addressed.
Received: 9 September 2018 / Revised: 8 October 2018 / Accepted: 11 October 2018 / Published: 19 October 2018
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Abstract

Recently, thiazolidinone derivatives have been widely studied as antiparasitic agents. Previous investigations showed that fused 4-thiazolidinone derivatives (especially thiopyranothiazoles) retain pharmacological activity of their synthetic precursors—simple 5-ene-4-thiazolidinones. A series of isothiochromeno[4a,4-d][1,3] thiazoles was investigated in an in vitro assay towards bloodstream forms of Trypanosoma brucei brucei. All compounds inhibited parasite growth at concentrations in the micromolar range. The established low acute toxicity of this class of compounds along with a good trypanocidal profile indicates that isothiochromenothiazole derivatives may be promising for designing new antitrypanosomal drugs. View Full-Text
Keywords: thiazolidinones; isothiochromenothiazoles; antitrypanosomal activity; Trypanosoma brucei; SAR analysis thiazolidinones; isothiochromenothiazoles; antitrypanosomal activity; Trypanosoma brucei; SAR analysis
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).
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Kryshchyshyn, A.; Kaminskyy, D.; Nektegayev, I.; Grellier, P.; Lesyk, R. Isothiochromenothiazoles—A Class of Fused Thiazolidinone Derivatives with Established Anticancer Activity That Inhibits Growth of Trypanosoma brucei brucei. Sci. Pharm. 2018, 86, 47.

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