Synthesis and biological evaluation of novel lignan glycosides as anticancer agents. (8th June 2016)

• Record Type: Journal Article
• Authors: Wang, Ying; Xia, Chao; Zhang, Wei; Zhao, Yu
• Is Part Of: Chemical biology & drug design. Volume 88:Number 4(2016)
• Page Start: 562
• Page End: 567
• Publication Date: 2016-06-08
• Subjects: inhibitors -- lignan glycosides -- synthesis -- vacuolar H + ‐ATPase; Drugs -- Design -- Periodicals; Pharmaceutical chemistry -- Periodicals; Biochemistry -- Periodicals; 615.19005
• DOI: 10.1111/cbdd.12785
• Languages: English
• ISSNs: 1747-0277

Abstract

Abstract : Novel lignan glycosides1a –1 h as analogues of cleistanthin A were designed and synthesized. Most of these compounds displayed significant cytotoxicities against four cancer cell lines. Compound1e displayed better cytotoxicity than cleistanthin A with IC50 values from 1.0 nm to 8.3 nm . Further lysosome acidity assay disclosed that1e could totally inhibit the activity of V‐ATPase at 60 nm . Abstract : Eight lignan glycosides were synthesized. Compound1e displayed strong cytotoxicity and V‐ATPase inhibitory activity.