Synthesis and in Vitro Evaluation of New Nitro-Substituted Thiazolyl Hydrazone Derivatives as Anticandidal and Anticancer Agents

Molecules

Ahmet Özdemir¹  Mehlika Dilek Altıntop¹  Gülhan Turan-Zitouni¹  Zafer Asım Kaplancıklı¹  Sinem Ilgın²  Özlem Atlı²  Fatih Demirci³ 

[1] Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Anadolu University,26470 Eskişehir, Turkey;Department of Pharmaceutical Toxicology, Faculty of Pharmacy, Anadolu University,26470 Eskişehir, Turkey;Graduate School of Health Sciences, Anadolu University, 26470 Eskişehir, Turkey;

关键词: thiazole;    hydrazone;    furan;    anticancer activity;    anticandidal activity;   

DOI  :  10.3390/molecules190914809

来源: DOAJ

【 摘 要 】

Fourteen new thiazolyl hydrazone derivatives were synthesized and evaluated for their anticandidal activity using a broth microdilution assay. Among thesynthesized 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 (IC50 = 125 µg/mL) and relatively low toxicity towards the NIH/3T3 cell line (IC50 > 500 µg/mL).

【 授权许可】

Unknown