title: Synthesis and biological evaluation of novel lignan glycosides as anticancer agents.
abstract: Novel lignan glycosides 1a-1 h as analogues of cleistanthin A were designed and synthesized. Most of these compounds displayed significant cytotoxicities against four cancer cell lines. Compound 1e displayed better cytotoxicity than cleistanthin A with IC50 values from 1.0 nm to 8.3 nm. Further lysosome acidity assay disclosed that 1e could totally inhibit the activity of V-ATPase at 60 nm.
authors.affiliation: School of Pharmacy, Nantong University, Nantong, China.|Institute of Nautical Medicine, Nantong University, Nantong, China.
authors.forename: Ying
authors.initials: Y
authors.lastname: Wang
authors.affiliation: School of Pharmacy, Nantong University, Nantong, China.
authors.forename: Chao
authors.initials: C
authors.lastname: Xia
authors.affiliation: School of Pharmacy, Nantong University, Nantong, China.
authors.forename: Wei
authors.initials: W
authors.lastname: Zhang
authors.affiliation: School of Pharmacy, Nantong University, Nantong, China. zhaoyu@ntu.edu.cn.
authors.forename: Yu
authors.initials: Y
authors.lastname: Zhao
mesh_terms: D000251:Adenosine Triphosphatases / Q000378:metabolism; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects*; D004789:Enzyme Activation / Q000187:drug effects; D006027:Glycosides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D020128:Inhibitory Concentration 50; D017705:Lignans / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D015394:Molecular Structure
chemical_list: D000970:Antineoplastic Agents; D006027:Glycosides; D017705:Lignans; C010088:cleistanthin; D000251:Adenosine Triphosphatases
keywords: inhibitors; lignan glycosides; synthesis; vacuolar H + -ATPase