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1H-Tetrazol-5-amine and 1,3-thiazolidin-4-one derivatives containing 3-(trifluoromethyl)phenyl scaffold: Synthesis, cytotoxic and anti-HIV studies.

1H-Tetrazol-5-amine and 1,3-thiazolidin-4-one derivatives containing 3-(trifluoromethyl)phenyl scaffold: Synthesis, cytotoxic and anti-HIV studies.
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Bielenica A, Szulczyk D, Olejarz W, Madeddu S, Giliberti G, Materek IB, Koziol AE, Struga M,


Bielenica A, Szulczyk D, Olejarz W, Madeddu S, Giliberti G, Materek IB, Koziol AE, Struga M, (click to view)

Bielenica A, Szulczyk D, Olejarz W, Madeddu S, Giliberti G, Materek IB, Koziol AE, Struga M,

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Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie 2017 08 0994() 804-812 pii 10.1016/j.biopha.2017.07.152

Abstract

On the basis of recently reported biologically active 3-(trifluoromethyl)phenylthioureas, a series of diaryl derivatives incorporating 1H-tetrazol-5-yl (1a-11a, 1a’-11a’) and 1,3-thiazolidin-4-one (1b-11b) scaffolds were synthesized. The synthesis pathway was confirmed by an X-ray crystallographic studies of 3a’, 6a, 8a, 6b and 8b. The cytotoxicity against MT-4 cells and anti-HIV properties of new derivatives were evaluated. As compared to initial thiourea connections, the cyclisation reduced the cytotoxicity of compounds by 2-15 times. The most promising N-(4-nitrophenyl)-1H-tetrazol-5-amine 7a was found to be more active than the origin thiourea. Its cytotoxicity was evaluated on A549, HTB-140 and HaCaT cell lines using MTT assay. The compound shows significant influence on cancer, but not on normal cells. Obtained results can provide some constructive data for further designing of novel family of potentially bioactive analogs.

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