Institution: | 1. Department of Chemistry, Düzce University, Faculty of Art & Sciences, 81620 Düzce, Türkiye
Department of Chemistry, Sakarya University, Faculty of Sciences, Department of Chemistry, 54187 Sakarya, Türkiye;2. Department of Medical Biology, Düzce University, Faculty of Medicine, 81620 Düzce, Türkiye;3. Department of Medical Biochemistry, Düzce University, Faculty of Medicine, 81620 Düzce, Türkiye;4. Department of Chemistry, Düzce University, Faculty of Art & Sciences, 81620 Düzce, Türkiye |
Abstract: | Methoxy group enriched eight coumarin-chalcone hybrid derivatives were synthesized. Antimicrobial/ antiproliferative activities were tested against eight human pathogenic microorganisms and four cancer cell lines (AGS, HepG2, MCF-7 and PC-3), respectively. Antimicrobial results showed that most of the compounds were almost more active than used standard antibiotics. Cytotoxicity results showed that 2,3,4-trimethoxyphenyl and thiophene containing structures have promising antiproliferative effects against AGS gastric cell lines with ~5 μg/ml IC50 values. At the same time, 2,4-dimethoxyphenyl bearing derivative exhibited the lowest IC50 values against HepG2 (~10 μg/ml) and PC-3 (~5 μg/ml) cell lines. Particularly, the cell viabilities of MCF-7 cell lines were remarkably inhibited by all the compounds with lower IC50 values. Therefore, molecular docking studies between hybrid ligands and quinone reductase-2 enzyme (regulates in MCF-7 cancer cells) were performed. The results demonstrated that all the derivatives can smoothly interact with interested enzyme in agreement with the experimental results. Finally, ADME parameters were studied to reveal drug-likeness potentials of the coumarin-chalcone hybrids. |