title: 3-O-Glutaryl-dihydrobetulin and related monoacyl derivatives as potent anti-HIV agents.
abstract: 3-O-Acyl-betulin and -dihydrobetulin derivatives were prepared and evaluated for anti-HIV activity. 3-O-Glutaryl-dihydrobetulin (17) demonstrated extremely potent anti-HIV activity with an EC(50) value of 2 x 10(-5) microM and a TI value of 1.12 x 10(6). 3-O-(3',3'-Dimethylsuccinyl)- and 3-O-(3',3'-dimethylglutaryl)-dihydrobetulins (15, 16) were also potent anti-HIV compounds with EC(50) values of 0.0017 and 0.0013 microM, respectively, and TI values of 16,160 and 19,530, respectively.
authors.affiliation: Faculty of Pharmaceutical Sciences, Niigata University of Pharmacy and Applied Life Sciences, Niigata 950-2081, Japan. kasiwada@niigata-pharm.ac.jp
authors.forename: Yoshiki
authors.initials: Y
authors.lastname: Kashiwada
authors.forename: Michiko
authors.initials: M
authors.lastname: Sekiya
authors.forename: Yasumasa
authors.initials: Y
authors.lastname: Ikeshiro
authors.forename: Toshihiro
authors.initials: T
authors.lastname: Fujioka
authors.forename: Nicole R
authors.initials: NR
authors.lastname: Kilgore
authors.forename: Carl T
authors.initials: CT
authors.lastname: Wild
authors.forename: Graham P
authors.initials: GP
authors.lastname: Allaway
authors.forename: Kuo-Hsiung
authors.initials: KH
authors.lastname: Lee
mesh_terms: D019380:Anti-HIV Agents / Q000737:chemistry* / Q000494:pharmacology*; D015497:HIV-1 / Q000187:drug effects* / Q000502:physiology; D006801:Humans; D014315:Triterpenes / Q000737:chemistry* / Q000494:pharmacology*; D000094062:Betulinic Acid
chemical_list: D019380:Anti-HIV Agents; D014315:Triterpenes; C098641:dihydrobetulinic acid; D000094062:Betulinic Acid