title: Synthesis and antitumor activity evaluation of novel oleanolic acid derivatives.
abstract: Ten novel oleanolic acid (OA) derivatives were synthesized through modifications at positions of A ring and C-28. Inhibitory activities of the oleanolic acid derivatives against SGC7901 and A549 cell lines were evaluated and confirmed by the tetrazolium bromidesalt (MTT) assay. The lab results revealed that all these compounds displayed some antitumor activity against SGC-7901 and A-549 cell lines. Among them, II4and II5exhibited excellent antitumor activities against SGC7901 cells and A549 cells, compared with gefitinib. Molecular docking studies have shown that compounds II4and II5produce potent antitumor activities by interacting with C-kit receptor through hydrogen bonds and hydrophobic bonds.
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: Yu-Wei
authors.initials: YW
authors.lastname: Zhao
authors.affiliation: a Department of Pharmaceutical Engineering , Shenyang University of Chemical Technology , Shenyang 110142 , China.
authors.forename: Zhen-Yu
authors.initials: ZY
authors.lastname: Kuai
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: Wei
authors.initials: W
authors.lastname: Li
mesh_terms: D000072283:A549 Cells; D000970:Antineoplastic Agents / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology*; D049109:Cell Proliferation / Q000187:drug effects; D004354:Drug Screening Assays, Antitumor; D000077156:Gefitinib; D006367:HeLa Cells; D006801:Humans; D062105:Molecular Docking Simulation; D015394:Molecular Structure; D009828:Oleanolic Acid / Q000031:analogs & derivatives / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D053978:Pentacyclic Triterpenes / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology*; D019009:Proto-Oncogene Proteins c-kit / Q000378:metabolism; D011799:Quinazolines / Q000494:pharmacology; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D053978:Pentacyclic Triterpenes; D011799:Quinazolines; D009828:Oleanolic Acid; D019009:Proto-Oncogene Proteins c-kit; D000077156:Gefitinib
keywords: Oleanolic acid; antitumor activity; pentacyclic triterpenoid