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Anti-Cancer Agents in Medicinal Chemistry


ISSN (Print): 1871-5206
ISSN (Online): 1875-5992

Research Article

Design, Synthesis and Biological Evaluation of 4, 6-Coumarin Derivatives as Anti- Cancer and Apoptosis-Inducing Agents

Author(s): Guoyi Yan, Jiang Luo , Xuan Han, Wenjuan Zhang , Chunlan Pu, Meng Zhou, Xinxin Zhong, Xueyan Hou, Man Zhou Hou and Rui Li *

Volume 21, Issue 17, 2021

Published on: 28 January, 2021

Page: [2351 - 2367] Pages: 17

DOI: 10.2174/1871520621666210129093857

Price: $65


Background: Coumarin structures were widely employed in anti-cancer drug design. Herein we focused on the modifications of C4 and C6 positions on coumarin scaffold to get novel anti-cancer agents.

Objective: The objective of the current work was the synthesis and biological evaluation of a series of 4, 6-coumarin derivatives to get novel anticancer agents.

Methods: Thirty-seven coumarin derivatives were designed and synthesized, the antiproliferative activity of the compounds was evaluated against human cancer cell lines and non-cancerous cells by MTT assay. The bioactivities and underlying mechanisms of active molecules were studied and the ADMET characters were predicted.

Results: Among the compounds, 4-p-hydroxy phenol-6-pinacol borane coumarin (25) exhibited a promising anti- cancer activity to cancer cell lines in a dose-dependent manner and the toxicity to normal cells was low. The mechanism of action was observed by inducing G2/M phase arrest and apoptosis which was further confirmed via western blot. In silico ADMET prediction revealed that compound 25 is a drug-like small molecule with a favorable safety profile.

Conclusion: The findings in this work may give vital information for further development of 6-pinacol borane coumarin derivatives as novel anti-cancer agents.

Keywords: Coumarin derivatives, structural optimization, anti-cancer agents, MTT assay, apoptosis, antiproliferative activity.

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