Antimicrobial, Antiproliferative Effects and Docking Studies of Methoxy Group Enriched Coumarin-Chalcone Hybrids.
Chem Biodivers
; 20(3): e202200973, 2023 Mar.
Article
in En
| MEDLINE
| ID: mdl-36691991
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 â¼5â
µg/ml IC50 values. At the same time, 2,4-dimethoxyphenyl bearing derivative exhibited the lowest IC50 values against HepG2 (â¼10â
µg/ml) and PC-3 (â¼5â
µg/ml) cell lines. Particularly, the cell viabilities of MCF-7â
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.
Key words
Full text:
1
Collection:
01-internacional
Database:
MEDLINE
Main subject:
Chalcone
/
Chalcones
/
Anti-Infective Agents
/
Antineoplastic Agents
Limits:
Humans
Language:
En
Journal:
Chem Biodivers
Journal subject:
BIOQUIMICA
/
QUIMICA
Year:
2023
Type:
Article