title: Betulinic Acid and its Derivatives as Potential Antitumor Agents.
abstract: Betulinic acid (BA) is a lupane-type pentacyclic triterpene, distributed ubiquitously throughout the plant kingdom. BA and its derivatives demonstrate multiple bioactivities, particularly an antitumor effect. This review critically describes the recent research on isolation, synthesis, and derivatization of BA and its natural analogs betulin and 23-hydroxybetulinic acid. The subsequent part of the review focuses on the current knowledge of antitumor properties, combination treatments, and pharmacological mechanisms of these compounds. A 3D-QSAR analysis of 62 BA derivatives against human ovarian cancer A2780 is also included to provide information concerning the structure-cytotoxicity relationships of these compounds.
authors.affiliation: Guangdong Province Key Laboratory of Pharmacodynamic Constituents of Traditional Chinese Medicine and New Drugs Research, College of Pharmacy, Jinan University, Guangzhou, 510632, P. R. China.
authors.forename: Dong-Mei
authors.initials: DM
authors.lastname: Zhang
authors.affiliation: Department of Medicinal Chemistry, College of Pharmacy, Jinan University, Guangzhou, 510632, P. R. China.
authors.forename: Hong-Gui
authors.initials: HG
authors.lastname: Xu
authors.affiliation: Guangdong Province Key Laboratory of Pharmacodynamic Constituents of Traditional Chinese Medicine and New Drugs Research, College of Pharmacy, Jinan University, Guangzhou, 510632, P. R. China.
authors.forename: Lei
authors.initials: L
authors.lastname: Wang
authors.affiliation: Guangdong Province Key Laboratory of Pharmacodynamic Constituents of Traditional Chinese Medicine and New Drugs Research, College of Pharmacy, Jinan University, Guangzhou, 510632, P. R. China.
authors.forename: Ying-Jie
authors.initials: YJ
authors.lastname: Li
authors.affiliation: Department of Medicinal Chemistry, College of Pharmacy, Jinan University, Guangzhou, 510632, P. R. China.
authors.forename: Ping-Hua
authors.initials: PH
authors.lastname: Sun
authors.affiliation: Institute of Pharmaceutical Research, College of Pharmacy, China Pharmaceutical University, Nanjing, 210009, P. R. China.
authors.forename: Xiao-Ming
authors.initials: XM
authors.lastname: Wu
authors.affiliation: Institute of Pharmaceutical Research, College of Pharmacy, China Pharmaceutical University, Nanjing, 210009, P. R. China.
authors.forename: Guang-Ji
authors.initials: GJ
authors.lastname: Wang
authors.affiliation: Department of Medicinal Chemistry, College of Pharmacy, Jinan University, Guangzhou, 510632, P. R. China.
authors.forename: Wei-Min
authors.initials: WM
authors.lastname: Chen
authors.affiliation: Guangdong Province Key Laboratory of Pharmacodynamic Constituents of Traditional Chinese Medicine and New Drugs Research, College of Pharmacy, Jinan University, Guangzhou, 510632, P. R. China.
authors.forename: Wen-Cai
authors.initials: WC
authors.lastname: Ye
mesh_terms: D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D053978:Pentacyclic Triterpenes; D021281:Quantitative Structure-Activity Relationship; D014315:Triterpenes / Q000737:chemistry / Q000494:pharmacology*; D000094062:Betulinic Acid
chemical_list: D000970:Antineoplastic Agents; D053978:Pentacyclic Triterpenes; D014315:Triterpenes; D000094062:Betulinic Acid
keywords: antitumor effect; betulinic acid; derivatives; structure-cytotoxicity relationship