Antimicrobial, Antiproliferative Effects and Docking Studies of Methoxy Group Enriched Coumarin-Chalcone Hybrids
Yükleniyor...
Dosyalar
Tarih
2023
Dergi Başlığı
Dergi ISSN
Cilt Başlığı
Yayıncı
John Wiley and Sons Inc
Erişim Hakkı
info:eu-repo/semantics/closedAccess
Özet
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 ?g/ml IC50 values. At the same time, 2,4-dimethoxyphenyl bearing derivative exhibited the lowest IC50 values against HepG2 (?10 ?g/ml) and PC-3 (?5 ?g/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. © 2023 Wiley-VHCA AG, Zurich, Switzerland.
Açıklama
Anahtar Kelimeler
antimicrobial, cancer, chalcone, coumarin, molecular docking, antineoplastic agent, chalcone, chalcone derivative, coumarin derivative, cell proliferation, chemical structure, chemistry, drug screening, human, MCF-7 cell line, molecular docking, structure activity relation, Antineoplastic Agents, Cell Proliferation, Chalcone, Chalcones, Coumarins, Drug Screening Assays, Antitumor, Humans, MCF-7 Cells, Molecular Docking Simulation, Molecular Structure, Structure-Activity Relationship
Kaynak
Chemistry and Biodiversity
WoS Q Değeri
Q3
Scopus Q Değeri
Q2
Cilt
20
Sayı
3
