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

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