[HTML][HTML] Synthesis and in vitro evaluation of new nitro-substituted thiazolyl hydrazone derivatives as anticandidal and anticancer agents

MD Altıntop, A Özdemir, G Turan-Zitouni, S Ilgın, Ö Atlı… - Molecules, 2014 - mdpi.com
Fourteen new thiazolyl hydrazone derivatives were synthesized and evaluated for their
anticandidal activity using a broth microdilution assay. Among the synthesized compounds,
2-[2-((5-(4-chloro-2-nitrophenyl) furan-2-yl) methylene) hydrazinyl]-4-(4-fluorophenyl)
thiazole and 2-[2-((5-(4-chloro-2-nitrophenyl) furan-2-yl) methylene) hydrazinyl]-4-(4-
methoxyphenyl) thiazole were found to be the most effective antifungal compounds against
Candida utilis, with a MIC value of 250 µg/mL, when compared with fluconazole (MIC= 2 …
Fourteen new thiazolyl hydrazone derivatives were synthesized and evaluated for their anticandidal activity using a broth microdilution assay. Among the synthesized compounds, 2-[2-((5-(4-chloro-2-nitrophenyl) furan-2-yl) methylene) hydrazinyl]-4-(4-fluorophenyl) thiazole and 2-[2-((5-(4-chloro-2-nitrophenyl) furan-2-yl) methylene) hydrazinyl]-4-(4-methoxyphenyl) thiazole were found to be the most effective antifungal compounds against Candida utilis, with a MIC value of 250 µg/mL, when compared with fluconazole (MIC= 2 µg/mL). Additionally, the synthesized compounds were evaluated for their in vitro cytotoxic effects on the MCF-7 and NIH/3T3 cell lines. As a result, 2-[2-((5-(4-chloro-2-nitrophenyl) furan-2-yl) methylene) hydrazinyl]-4-(4-chlorophenyl) thiazole was identified as the most promising anticancer compound against MCF-7 cancer cells due to its inhibitory effects (IC 50= 125 µg/mL) and relatively low toxicity towards the NIH/3T3 cell line (IC 50> 500 µg/mL).
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