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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
来源:
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).
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页码:14809 / 14820
页数:12
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