2. Academic Validation
  3. 2-Benzoylbenzofuran derivatives possessing piperazine linker as anticancer agents

2-Benzoylbenzofuran derivatives possessing piperazine linker as anticancer agents

  • Bioorg Med Chem Lett. 2019 Mar 15;29(6):806-810. doi: 10.1016/j.bmcl.2019.01.025.
Hui Gao 1,  Xia Zhang 1,  Xiao-Jia Pu 1,  Xi Zheng 2,  Bei Liu 1,  Gao-Xiong Rao 1,  Chun-Ping Wan 3,  Ze-Wei Mao 4
Affiliations

Affiliations

  • 1 College of Pharmaceutical Science, Yunnan University of Traditional Chinese Medicine, Kunming 650500, PR China.
  • 2 Central Laboratory, The NO. 1 Affiliated Hospital of Yunnan University of Traditional Chinese Medicine, Kunming 650021, PR China.
  • 3 Central Laboratory, The NO. 1 Affiliated Hospital of Yunnan University of Traditional Chinese Medicine, Kunming 650021, PR China. Electronic address: wanchunping1012@163.com.
  • 4 College of Pharmaceutical Science, Yunnan University of Traditional Chinese Medicine, Kunming 650500, PR China. Electronic address: maozw@ynutcm.edu.cn.
PMID: 30709651 DOI: 10.1016/j.bmcl.2019.01.025
Abstract

A series of novel 2-benzoylbenzofuran derivatives possessing piperazine linker have been prepared, and their in vitro Anticancer activity against a panel of human tumor cell lines by MTT assay were evaluated. The results demonstrated that tertiary amine derivatives exhibited better cytotoxic activity, and SAR study revealed that electron-donating substituents on the phenyl ring of the derivatization functionality contributed to potent Anticancer activities. Among them, compounds 6, 9, 11, 18, 23 and 25 displayed both better anti-tumor activity and lower cytotoxic effect on human normal liver cell L02. Further Apoptosis analysis showed that compound 18 significantly induced Apoptosis in A549 cell, which was considered as the most potent Anticancer agent.

Keywords

2-Benzoylbenzofuran; Anticancer activity; Apoptosis; Cytotoxicity.

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