2-Benzoylbenzofuran derivatives possessing piperazine linker as anticancer agents. Issue 6 (15th March 2019)

• Record Type: Journal Article
• Authors: Gao, Hui; Zhang, Xia; Pu, Xiao-Jia; Zheng, Xi; Liu, Bei; Rao, Gao-Xiong; Wan, Chun-Ping; Mao, Ze-Wei
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 29:Issue 6(2019)
• Page Start: 806
• Page End: 810
• Publication Date: 2019-03-15
• Subjects: 2-Benzoylbenzofuran -- Anticancer activity -- Cytotoxicity -- Apoptosis; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2019.01.025
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: A series of novel 2-benzoylbenzofuran derivatives possessing piperazine linker have been designed and synthesized, and in vitro anticancer activities against five human cancer cell lines were evaluated. The results demonstrated that tertiary amine compounds 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, many compounds displayed lower cytotoxic effect on human normal liver cell L02. Further apoptosis analysis indicated that compound18 could induced apoptosis on A549 cell. 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, compounds6, 9, 11, 18, 23 and25 displayed both better anti-tumor activity and lower cytotoxic effect on human normal liver cell L02. Further apoptosis analysis showed that compound18 significantly induced apoptosis in A549 cell, which was considered as the most potent anticancer agent.