title: Synthesis and antiproliferative evaluation of 23-hydroxybetulinic acid derivatives.
abstract: Based on structural modifications of the natural 23-hydroxybetulinic acid, a series of novel its derivatives had been synthesized. The new compounds were screened for in vitro antiproliferative activity against cancer cell lines HeLa, MCF-7, HepG2, B16 and A375 using doxorubicin as a reference. The vast majority of derivatives had exhibited potent tumor growth inhibitory activity than original compound. The derivatives 4, 5, 7, 20, 23, 26, 43 and 44 with IC50 values lower than 10 μM on all tested cell lines were regarded as the most promising compounds. The structure-activity relationships of 23-hydroxybetulinic acid derivatives were also discussed in the present investigations.
authors.affiliation: Guangdong Province Key Laboratory of Pharmacodynamic Constituents of TCM and New Drugs Research, College of Pharmacy, Jinan University, Guangzhou 510632, PR China.
authors.forename: Ping
authors.initials: P
authors.lastname: Lan
authors.forename: Jiao
authors.initials: J
authors.lastname: Wang
authors.forename: Dong-Mei
authors.initials: DM
authors.lastname: Zhang
authors.forename: Chang
authors.initials: C
authors.lastname: Shu
authors.forename: Hui-Hui
authors.initials: HH
authors.lastname: Cao
authors.forename: Ping-Hua
authors.initials: PH
authors.lastname: Sun
authors.forename: Xiao-Ming
authors.initials: XM
authors.lastname: Wu
authors.forename: Wen-Cai
authors.initials: WC
authors.lastname: Ye
authors.forename: Wei-Min
authors.initials: WM
authors.lastname: Chen
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D049109:Cell Proliferation / Q000187:drug effects; D002470:Cell Survival / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D006367:HeLa Cells; D006801:Humans; D015394:Molecular Structure; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D014315:Triterpenes / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D014407:Tumor Cells, Cultured
chemical_list: C468651:23-hydroxybetulinic acid; D000970:Antineoplastic Agents; D014315:Triterpenes