Infertility affects 15% of couples worldwide as the disease of the reproductive system and 30%-50% of infertile cases are related to male-dependent factors (Ghuman & Ramalingam, 2017; 'Mother or nothing: the agony of infertility', 2010). Recent studies have shown that sperm quality is decreasing all over the world. The exact cause of this situation has not been fully understood; however, chronic exposures to chemicals especially drugs take an important place (Gabrielsen & Tanrikut, 2016). The complex aetiology underlying male-factor infertility makes it harder to understand at what level drug exposures are responsible for it. Additionally, the number of chronic disease cases, such as migraine, depression, and epilepsy, is increasing year by year, pointing out the fact that long-term drug exposures become frequently because of the need of treating these diseases at younger ages (Kristensen, 2018). Schizophrenia is a serious psychiatric disorder, results in longterm antipsychotic treatment. Today, atypical antipsychotics are the
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. Methods: 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.
A series of novel chalcone derivatives bearing diverse heterocycles have been synthesized and evaluated for their antiproliferative activity against A549 (human lung adenocarcinoma) and C6 (rat brain glioma) cells. Structures of the title compounds (3-18) were verified by FT-IR, 1H NMR, 13C NMR, HRMS spectral data and elemental analyses. Antiproliferative activities of the compounds were evaluated using MTT assay, BrdU method, and flow cytometric analysis. Compounds 9 and 15 were revealed as the most promising cytotoxic agents due to their selectivity towards A549 cells with a lower IC50 values (IC50=0.05 µM and IC50=0.0316 µM) than cisplatin (IC50=0.06 µM). Flow cytometric analysis of compounds 9 and 15 showed that they affected lung cancer cells by the apoptotic pathway.
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