title: Synthesis and pro-apoptotic activity of novel glycyrrhetinic acid derivatives.
abstract: Triterpenoids are used for medicinal purposes in many countries. Some, such as oleanolic and glycyrrhetinic acids, are known to be anti-inflammatory and anticarcinogenic. However, the biological activities of these naturally occurring molecules against their particular targets are weak, so the synthesis of new synthetic analogues with enhanced potency is needed. By combining modifications to both the A and C rings of 18βH-glycyrrhetinic acid, the novel synthetic derivative methyl 2-cyano-3,12-dioxo-18βH-olean-9(11),1(2)-dien-30-oate was obtained. This derivative displays high antiproliferative activity in cancer cells, including a cell line with a multidrug-resistance phenotype. It causes cell death by inducing the intrinsic caspase-dependent apoptotic pathway.
authors.affiliation: Institute of Chemical Biology and Fundamental Medicine, Siberian Branch, Russian Academy of Sciences, 8, Lavrent'ev avenue, 630090 Novosibirsk, Russian Federation. evg_log@niboch.nsc.ru
authors.forename: Evgeniya B
authors.initials: EB
authors.lastname: Logashenko
authors.forename: Oksana V
authors.initials: OV
authors.lastname: Salomatina
authors.forename: A V
authors.initials: AV
authors.lastname: Markov
authors.forename: Dina V
authors.initials: DV
authors.lastname: Korchagina
authors.forename: Nariman F
authors.initials: NF
authors.lastname: Salakhutdinov
authors.forename: Genrikh A
authors.initials: GA
authors.lastname: Tolstikov
authors.forename: Valentin V
authors.initials: VV
authors.lastname: Vlassov
authors.forename: Marina A
authors.initials: MA
authors.lastname: Zenkova
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects*; D045744:Cell Line, Tumor; D006034:Glycyrrhetinic Acid / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology*; D006035:Glycyrrhiza / Q000737:chemistry*; D006801:Humans; D009369:Neoplasms / Q000188:drug therapy
chemical_list: D000970:Antineoplastic Agents; D006034:Glycyrrhetinic Acid