title: Synthesis of novel oleanolic acid and ursolic acid in C-28 position derivatives as potential anticancer agents.
abstract: A series of nitrogen-containing derivatives of oleanolic acid and ursolic acid were prepared by a modification at C-28 position via esterification with 2-hydroxyacetic acid followed by amidation with amines, such as piperazine, N-methylpiperazine, and alkane-1, 2-diamines, alkane-1, 4-diamines, alkane-1, 6-diamines. In vitro antiproliferative activities of the compounds prepared towards MCF-7, Hela and A549 cell lines were evaluated by a MTT method to show that OA-5a, OA-5b, OA-5c and UA-5a showed somewhat improved antiproliferative activities against MCF-7, Hela and A549 cells comparing to that of the positive control, gefitinib.
authors.affiliation: School of Chemistry and Chemical Engineering, Liaoning Normal University, Dalian, 116-029, Liaoning, People's Republic of China.
authors.forename: Tian
authors.initials: T
authors.lastname: Tian
authors.affiliation: School of Chemistry and Chemical Engineering, Liaoning Normal University, Dalian, 116-029, Liaoning, People's Republic of China.
authors.forename: Xinyu
authors.initials: X
authors.lastname: Liu
authors.affiliation: College of Pharmacy, Yeungnam University, Kyongsan, 712-749, Korea.
authors.forename: Eung-Seok
authors.initials: ES
authors.lastname: Lee
authors.affiliation: School of Chemistry and Chemical Engineering, Liaoning Normal University, Dalian, 116-029, Liaoning, People's Republic of China.
authors.forename: Jingyang
authors.initials: J
authors.lastname: Sun
authors.affiliation: School of Chemistry and Chemical Engineering, Liaoning Normal University, Dalian, 116-029, Liaoning, People's Republic of China.
authors.forename: Zhonghua
authors.initials: Z
authors.lastname: Feng
authors.affiliation: School of Chemistry and Chemical Engineering, Liaoning Normal University, Dalian, 116-029, Liaoning, People's Republic of China. lxzhao@lnnu.edu.cn.|Liaoning Provincial Key Laboratory of Biotechnology and Drug Discovery, Liaoning Normal University, Dalian, 116-029, Liaoning, People's Republic of China. lxzhao@lnnu.edu.cn.
authors.forename: Longxuan
authors.initials: L
authors.lastname: Zhao
authors.affiliation: Liaoning Provincial Key Laboratory of Biotechnology and Drug Discovery, Liaoning Normal University, Dalian, 116-029, Liaoning, People's Republic of China. zch@lnnu.edu.cn.
authors.forename: Chunhui
authors.initials: C
authors.lastname: Zhao
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D006367:HeLa Cells; D006801:Humans; D061986:MCF-7 Cells; D015394:Molecular Structure; D009828:Oleanolic Acid / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D014315:Triterpenes / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D000097245:Ursolic Acid
chemical_list: D000970:Antineoplastic Agents; D009828:Oleanolic Acid; D014315:Triterpenes; D000097245:Ursolic Acid
keywords: Antiproliferative activity; Oleanolic acid; Structure–activity relationships; Ursolic acid