Discovery of novel bis-evodiamine derivatives with potent antitumor activity. (1st July 2022)

• Record Type: Journal Article
• Authors: Liang, Huixin; Wang, Wei; Zhu, Fugui; Chen, Shuqiang; Liu, Dan; Sheng, Chunquan
• Is Part Of: Bioorganic & medicinal chemistry. Volume 65(2022)
• Publication Date: 2022-07-01
• Subjects: Bis-evodiamine -- Twin drug -- Antitumor activity -- Apoptosis; NPs natural products -- AChE acetylcholinesterase -- SAR structure-activity relationship -- EDCI 1-ethyl-3-(3-dimethylaminopropyl) carbodiimide hydrochloride -- DMAP 4-dimethylaminopyridine -- CCK-8 cell counting kit-8 -- CPT camptothecin -- HUVEC human umbilical vein endothelial cells -- RTCA real-time cell analysis; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; Biochemistry -- Periodicals; Chemistry, Clinical -- Periodicals; Chemistry, Organic -- Periodicals; Chimie bio-organique -- Périodiques; Chimie pharmaceutique -- Périodiques; 615.19
• DOI: 10.1016/j.bmc.2022.116793
• Languages: English
• ISSNs: 0968-0896

Abstract

Graphical abstract: Inspired by antitumor natural product evodiamine, a series of novel bis-evodiamine derivatives were designed and synthesized, which showed potent antitumor activity. Abstract: Inspired by antitumor natural product evodiamine, a series of novel bis-evodiamine derivatives were designed and synthesized, which showed potent antitumor activity. In particular, compound 13b effectively inhibited the proliferation and migration of HCT116 cells. Further mechanism studies revealed that compound 13b acted by inducing HCT116 cell apoptosis and arresting the cell cycle at the G2/M phase. Thus, compound 13b represents a promising lead compound for the discovery of novel antitumor agents.