title: Synthesis and antitumor activity evaluation of new asiatic acid derivatives.
abstract: Twelve novel asiatic acid (AA) derivatives were designed and synthesized. Their structures were confirmed using NMR, MS, and IR spectra. Their in vitro cytotoxicities on various cancer cell lines (HeLa, HepG2, BGC-823, and SKOV3) were evaluated by the 3-(4,5-dimethyl-2-thiazolyl)-2,5-diphenyl-2H-tetrazolium bromide assay. Most of the derivatives were found to have stronger cell growth inhibitory activity than AA. Among them, compounds 5-8 and 11 with substituted amide group at C-28 exhibited more potent cytotoxicity than AA, Gefitinib, and etoposide (positive control).
authors.affiliation: Department of Pharmaceutical Engineering, Shenyang University of Chemical Technology, Shenyang, China. mengyanqiu@hotmail.com
authors.forename: Yan-Qiu
authors.initials: YQ
authors.lastname: Meng
authors.forename: Yun-Yun
authors.initials: YY
authors.lastname: Li
authors.forename: Feng-Qing
authors.initials: FQ
authors.lastname: Li
authors.forename: Yan-Ling
authors.initials: YL
authors.lastname: Song
authors.forename: Hai-Feng
authors.initials: HF
authors.lastname: Wang
authors.forename: Hong
authors.initials: H
authors.lastname: Chen
authors.forename: Bo
authors.initials: B
authors.lastname: Cao
mesh_terms: D000972:Antineoplastic Agents, Phytogenic / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology*; D004354:Drug Screening Assays, Antitumor; D006367:HeLa Cells; D006801:Humans; D019906:Nuclear Magnetic Resonance, Biomolecular; D053978:Pentacyclic Triterpenes / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D000972:Antineoplastic Agents, Phytogenic; D053978:Pentacyclic Triterpenes; C017032:asiatic acid