title: Synthesis and biological evaluation of oleanolic acid derivatives as antitumor agents.
abstract: Derivatives of oleanolic acid were synthesized and evaluated in vitro for their growth inhibition against human hepatocellular carcinoma cell line (HepG2) and colon cancer cell line (Col-02). Several derivatives exhibited moderate-to-good inhibitory activity, with 3 displaying the most promising inhibition [GI₅₀ = 1.75 μM (HepG2), 0.71 μM (Col-02)]. Structure-activity relationship analyses of these derivatives demonstrated that a 1-en-2-cyano-3-oxo in ring A and a nitro at C-17 were important in retention of the inhibition against HepG2 and Col-02 cells.
authors.affiliation: Key Laboratory of Drug Targeting and Drug Delivery System of the Education Ministry, Department of Medicinal Chemistry, West China School of Pharmacy, Sichuan University, Chengdu 610041, China.
authors.forename: Lei
authors.initials: L
authors.lastname: Chen
authors.forename: Jian-Bo
authors.initials: JB
authors.lastname: Wu
authors.forename: Fan
authors.initials: F
authors.lastname: Lei
authors.forename: Shan
authors.initials: S
authors.lastname: Qian
authors.forename: Li
authors.initials: L
authors.lastname: Hai
authors.forename: Yong
authors.initials: Y
authors.lastname: Wu
mesh_terms: D000972:Antineoplastic Agents, Phytogenic / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D004354:Drug Screening Assays, Antitumor; D056945:Hep G2 Cells; D006801:Humans; D015394:Molecular Structure; D009828:Oleanolic Acid / Q000031:analogs & derivatives / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship
chemical_list: D000972:Antineoplastic Agents, Phytogenic; D009828:Oleanolic Acid