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

被引:44
作者
Altintop, Mehlika Dilek [1 ,2 ]
Ozdemir, Ahmet [1 ]
Turan-Zitouni, Gulhan [1 ]
Ilgin, Sinem [3 ]
Atli, Ozlem [3 ]
Demirci, Fatih [2 ,4 ]
Kaplancikli, Zafer Asim [1 ]
机构
[1] Anadolu Univ, Fac Pharm, Dept Pharmaceut Chem, TR-26470 Eskisehir, Turkey
[2] Anadolu Univ, Grad Sch Hlth Sci, TR-26470 Eskisehir, Turkey
[3] Anadolu Univ, Fac Pharm, Dept Pharmaceut Toxicol, TR-26470 Eskisehir, Turkey
[4] Anadolu Univ, Fac Pharm, Dept Pharmacognosy, TR-26470 Eskisehir, Turkey
关键词
thiazole; hydrazone; furan; anticancer activity; anticandidal activity; BIOLOGICAL-ACTIVITIES; ANTIPROLIFERATIVE ACTIVITY; ANTIFUNGAL AGENTS; DRUG-RESISTANCE; CANCER-CELLS; INFECTIONS; HYDRAZIDES; INHIBITORS; ANALOGS; MOIETY;
D O I
10.3390/molecules190914809
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
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 mu g/mL, when compared with fluconazole (MIC = 2 mu g/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 mu g/mL) and relatively low toxicity towards the NIH/3T3 cell line (IC50 > 500 mu g/mL).
引用
收藏
页码:14809 / 14820
页数:12
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