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Synthesis and in vitro evaluation of new nitro-substituted thiazolyl hydrazone derivatives as anticandidal and anticancer agents.
- Source :
-
Molecules (Basel, Switzerland) [Molecules] 2014 Sep 17; Vol. 19 (9), pp. 14809-20. Date of Electronic Publication: 2014 Sep 17. - Publication Year :
- 2014
-
Abstract
- 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 (IC50=125 µg/mL) and relatively low toxicity towards the NIH/3T3 cell line (IC50>500 µg/mL).
- Subjects :
- Animals
Antifungal Agents chemical synthesis
Antineoplastic Agents chemical synthesis
Drug Screening Assays, Antitumor
Humans
Hydrazones chemical synthesis
MCF-7 Cells
Mice
Microbial Sensitivity Tests
NIH 3T3 Cells
Thiazoles chemical synthesis
Antifungal Agents pharmacology
Antineoplastic Agents pharmacology
Candida drug effects
Hydrazones pharmacology
Thiazoles pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 1420-3049
- Volume :
- 19
- Issue :
- 9
- Database :
- MEDLINE
- Journal :
- Molecules (Basel, Switzerland)
- Publication Type :
- Academic Journal
- Accession number :
- 25232704
- Full Text :
- https://doi.org/10.3390/molecules190914809