title: Synthesis and in vitro evaluation of new nitro-substituted thiazolyl hydrazone derivatives as anticandidal and anticancer agents.
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).
authors.affiliation: Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Anadolu University, 26470 Eskişehir, Turkey. mdaltintop@anadolu.edu.tr.
authors.forename: Mehlika Dilek
authors.initials: MD
authors.lastname: Altıntop
authors.affiliation: Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Anadolu University, 26470 Eskişehir, Turkey.
authors.forename: Ahmet
authors.initials: A
authors.lastname: Özdemir
authors.affiliation: Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Anadolu University, 26470 Eskişehir, Turkey.
authors.forename: Gülhan
authors.initials: G
authors.lastname: Turan-Zitouni
authors.affiliation: Department of Pharmaceutical Toxicology, Faculty of Pharmacy, Anadolu University, 26470 Eskişehir, Turkey. silgin@anadolu.edu.tr.
authors.forename: Sinem
authors.initials: S
authors.lastname: Ilgın
authors.affiliation: Department of Pharmaceutical Toxicology, Faculty of Pharmacy, Anadolu University, 26470 Eskişehir, Turkey.
authors.forename: Özlem
authors.initials: Ö
authors.lastname: Atlı
authors.affiliation: Graduate School of Health Sciences, Anadolu University, 26470 Eskişehir, Turkey. fdemirci@anadolu.edu.tr.
authors.forename: Fatih
authors.initials: F
authors.lastname: Demirci
authors.affiliation: Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Anadolu University, 26470 Eskişehir, Turkey. zakaplan@anadolu.edu.tr.
authors.forename: Zafer Asım
authors.initials: ZA
authors.lastname: Kaplancıklı
mesh_terms: D000818:Animals; D000935:Antifungal Agents / Q000138:chemical synthesis / Q000494:pharmacology*; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000494:pharmacology*; D002175:Candida / Q000187:drug effects*; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D006835:Hydrazones / Q000138:chemical synthesis / Q000494:pharmacology*; D061986:MCF-7 Cells; D051379:Mice; D008826:Microbial Sensitivity Tests; D041681:NIH 3T3 Cells; D013844:Thiazoles / Q000138:chemical synthesis / Q000494:pharmacology*
chemical_list: D000935:Antifungal Agents; D000970:Antineoplastic Agents; D006835:Hydrazones; D013844:Thiazoles