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Letters in Drug Design & Discovery

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ISSN (Print): 1570-1808
ISSN (Online): 1875-628X

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Research Article

Design, Synthesis, and Antiproliferative Activity of Novel Flavone Derivatives

Author(s): Lata C. Potey*, Prafulla M. Sabale and Vidya P. Sabale

Volume 20, Issue 10, 2023

Published on: 28 October, 2022

Page: [1610 - 1620] Pages: 11

DOI: 10.2174/1570180819666220919124717

Price: $65

Abstract

Background: Cancer is a complex disease in which some of the cells grow uncontrollably and spread to other parts of the body.

Objective: The present study focuses on molecular docking and synthesis of novel flavone derivatives substituted with heterocyclic rings.

Methods: The anticancer activity of novel flavones against human aromatase enzyme using human breast cancer cell line MCF-7 through MTT assay was demonstrated. The synthesized compounds for the determination of single or double-strand DNA damage through the single-cell electrophoresis/comet assay were evaluated.

Results: In this study, we found that the derivative 3M with morpholine ring showed the highest anticancer potency against the MCF-7 cell line compared to that of other flavone derivatives. Compound 3T showed less cytotoxicity against the MCF-7 cell line.

Conclusion: Based on the findings, flavone scaffolds can be selected as a skeleton for the development of heterocyclic amine-containing flavones with the potential to develop as anticancer drugs.

Keywords: Flavones, cancer, breast cancer, MCF-7, cytotoxicity, Comet assay, MTT assay

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Graphical Abstract

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