Anticancer evaluation of benzofuran derivatives linked to dipiperazine moiety

Yixin Liu; Zhao Wu; Minxin Li; Hui Gao; Chunping Wan; Zewei Mao

doi:10.1016/j.bmcl.2023.129378

Anticancer evaluation of benzofuran derivatives linked to dipiperazine moiety

Bioorg Med Chem Lett. 2023 Jul 15:91:129378. doi: 10.1016/j.bmcl.2023.129378. Epub 2023 Jun 16.

Authors

Yixin Liu¹, Zhao Wu¹, Minxin Li¹, Hui Gao¹, Chunping Wan², Zewei Mao³

Affiliations

¹ School of Chinese Materia Medica, Yunnan University of Chinese Medicine, Kunming 650500, PR China.
² Central Laboratory, The NO.1 Affiliated Hospital of Yunnan University of Chinese Medicine, Kunming 650021, PR China. Electronic address: wanchunping1012@163.com.
³ School of Chinese Materia Medica, Yunnan University of Chinese Medicine, Kunming 650500, PR China. Electronic address: maozw@ynutcm.edu.cn.

PMID: 37330115
DOI: 10.1016/j.bmcl.2023.129378

Abstract

In this work, a series of novel benzofuran derivatives linked to dipiperazine moiety have been prepared, and in vitro anticancer activity against Hela and A549 was investigated. The results demonstrated that benzofuran derivatives exerted potent antitumor effect. Especially, compounds 8c and 8d showed better antitumor activity against A549 (IC₅₀ = 0.12 μM and 0.43 μM). Further mechanism study indicated that compound 8d could significantly induce cell apoptosis in A549 by FACs analysis.

Keywords: Anticancer; Apoptosis; Benzofuran; Dipiperazine.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Antineoplastic Agents* / pharmacology
Apoptosis
Benzofurans* / pharmacology
Cell Line, Tumor
Cell Proliferation
Drug Screening Assays, Antitumor
HeLa Cells
Humans
Molecular Structure
Structure-Activity Relationship

Substances

Antineoplastic Agents
Benzofurans