title: Synthesis and in vitro antitumor activities of lupeol dicarboxylic acid monoester derivatives.
abstract: Ten lupeol dicarboxylic acid monoester derivatives as new potent antitumor agents were synthesized and evaluated for in vitro antitumor activities against A549, LAC, HepG2 and HeLa cell lines. Among them, compounds 1-5 showed excellent antitumor activities against all tested tumor cell lines and compounds 6-10 exhibited high activities against A549, HepG2 and HeLa cells, exceeded lupeol, lupanol and doxorubicin. Compound 2 displayed the highest potent antitumor activities with IC50 values of 5.78 μM against A549 cell, 2.38 μM against LAC cell, 6.14 μM against HepG2 cell and 0.00842 μM against HeLa cell.
authors.affiliation: Department of Chemistry, Hanshan Normal University, Chaozhou, 521041, China, weijieli1688@yahoo.com.cn.
authors.forename: Weijie
authors.initials: W
authors.lastname: Li
authors.forename: Jing
authors.initials: J
authors.lastname: Hao
authors.forename: Yeyu
authors.initials: Y
authors.lastname: Xiao
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D003998:Dicarboxylic Acids / Q000138:chemical synthesis* / Q000494:pharmacology; D004354:Drug Screening Assays, Antitumor / Q000379:methods; D004365:Drugs, Chinese Herbal / Q000138:chemical synthesis* / Q000493:pharmacokinetics; D006367:HeLa Cells; D056945:Hep G2 Cells; D006801:Humans; D053978:Pentacyclic Triterpenes / Q000138:chemical synthesis* / Q000494:pharmacology; D013329:Structure-Activity Relationship; D000094042:Lupanes
chemical_list: D000970:Antineoplastic Agents; D003998:Dicarboxylic Acids; D004365:Drugs, Chinese Herbal; D053978:Pentacyclic Triterpenes; C010480:lupeol; D000094042:Lupanes