Background: In medicinal chemistry, thiazoles have gained great importance in antifungal
and anticancer drug design and development.
Objectives: The aim of this study was to synthesize new quinoline-based thiazolyl hydrazone
derivatives and evaluate their anticandidal and anticancer effects.
Methods: New thiazolyl hydrazone derivatives were evaluated for their anticandidal effects using
disc diffusion method. Ames MPF assay was carried out to determine the genotoxicity of the most
effective antifungal derivative. MTT assay was also performed to assess the cytotoxic effects of the
compounds on A549 human lung adenocarcinoma, HepG2 human hepatocellular carcinoma, MCF-
7 human breast adenocarcinoma and NIH/3T3 mouse embryonic fibroblast (healthy) cell lines.
Results: 4-(4-Fluorophenyl)-2-(2-((quinolin-4-yl)methylene)hydrazinyl)thiazole (4) showed antifungal
activity against Candida albicans and Candida krusei in the concentration of 1 mg/mL. In
MTT and Ames MPF tests, it was determined that compound 4 did not show cytotoxic and genotoxic
effects. MTT assay indicated that 4-(naphthalen-2-yl)-2-(2-((quinolin-4-yl)methylene)
hydrazinyl)thiazole (10) showed more selective anticancer activity than cisplatin against A549 and
MCF-7 cell lines. Besides, 4-(4-chlorophenyl)-2-(2-((quinolin-4-yl)methylene)hydrazinyl)thiazole
(5) exhibited more selective anticancer activity than cisplatin against HepG2 cell line.
Conclusion: Due to their high selectivity index, these compounds are considered as candidate compounds
to participate in further research.