title: Synthesis and antitumor activity evaluation of novel ursolic acid derivatives.
abstract: Eleven novel ursolic acid (UA) derivatives were designed and synthesized with modification at positions of C-2, C-3, and C-28 of UA. Their structures were confirmed by MS, (1)H NMR, and elemental analysis. Their in vitro cytotoxicities against various cancer cell lines (HeLa, HepG2, and BGC-823) were evaluated by MTT assay. The results indicated that all compounds could inhibit cell proliferation of HeLa, HepG2, and BGC-823 cells. Among them, compounds I3 and I4 showed more potent cytotoxicity on these three tumor cells than gefitinib (positive control), worthy to be studied further.
authors.affiliation: a Department of Pharmaceutical Engineering , Shenyang University of Chemical Technology , Shenyang 110142 , China.
authors.forename: Yan-Qiu
authors.initials: YQ
authors.lastname: Meng
authors.affiliation: a Department of Pharmaceutical Engineering , Shenyang University of Chemical Technology , Shenyang 110142 , China.
authors.forename: Liang-Feng
authors.initials: LF
authors.lastname: Zhang
authors.affiliation: a Department of Pharmaceutical Engineering , Shenyang University of Chemical Technology , Shenyang 110142 , China.
authors.forename: Dong-Ying
authors.initials: DY
authors.lastname: Liu
authors.affiliation: a Department of Pharmaceutical Engineering , Shenyang University of Chemical Technology , Shenyang 110142 , China.
authors.forename: Li-Wei
authors.initials: LW
authors.lastname: Liu
authors.affiliation: a Department of Pharmaceutical Engineering , Shenyang University of Chemical Technology , Shenyang 110142 , China.
authors.forename: Yi
authors.initials: Y
authors.lastname: Zhang
authors.affiliation: a Department of Pharmaceutical Engineering , Shenyang University of Chemical Technology , Shenyang 110142 , China.
authors.forename: Min-Jie
authors.initials: MJ
authors.lastname: Zhao
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D049109:Cell Proliferation / Q000187:drug effects; D004354:Drug Screening Assays, Antitumor; D006367:HeLa Cells; D056945:Hep G2 Cells; D006801:Humans; D015394:Molecular Structure; D019906:Nuclear Magnetic Resonance, Biomolecular; D014315:Triterpenes / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D000097245:Ursolic Acid
chemical_list: D000970:Antineoplastic Agents; D014315:Triterpenes; D000097245:Ursolic Acid
keywords: antitumor activity; synthesized; triterpenoid; ursolic acid derivatives