Title:Apigenin Bioisosteres: Synthesis and Evaluation of their Antioxidant, Antimicrobial, and Anticancer Activities
Volume: 21
Issue: 12
Author(s): Juhi Gupta, Kalyani Thombre, Krishna Gupta*Milind Umekar
Affiliation:
- Department of Pharmaceutical Chemistry, Smt. Kishoritai Bhoyar College of Pharmacy, Kamptee, Nagpur (MS), India
Keywords:
Flavonoids, apigenin, DPPH, disc diffusion assay, MCF-7 cell line, MTT.
Abstract: A novel series of Apigenin bioisosteres [1(4-chlorophenyl)-3-phenyl prop-2-ene-1-one]
non-cyclic derivatives (4a-4c) and [7-hydroxy-2-phenyl-4H-chromen-4-one] cyclic derivatives (9a-
9d) were synthesized. The newly synthesized apigenin bioisosteres were confirmed using UV, IR,
NMR, and mass spectroscopic methods. The antioxidant, antibacterial, and anti-cancer activities of all
newly synthesized compounds were assessed using the DPPH free radical scavenging capacity, disc
diffusion method, and in vitro MTT assay on the human breast cancer MCF-7 cell line. Almost all the
synthesized apigenin bioisosteres had greater antioxidant and antimicrobial activity than standard
Apigenin. Out of seven compounds (4a-4c and 9a-9d), five compounds were found to exhibit notable
antiproliferative activity on the breast cancer cell line (MCF-7), whereas two compounds, 9c and 9d,
did not show notable activity. Our analysis suggests that synthesized Apigenin bioisosteres function
as prospective antioxidant, antimicrobial, and anticancer agents.
