2. Academic Validation
  3. 3-O-Glutaryl-dihydrobetulin and related monoacyl derivatives as potent anti-HIV agents

3-O-Glutaryl-dihydrobetulin and related monoacyl derivatives as potent anti-HIV agents

  • Bioorg Med Chem Lett. 2004 Dec 6;14(23):5851-3. doi: 10.1016/j.bmcl.2004.09.033.
Yoshiki Kashiwada 1,  Michiko Sekiya,  Yasumasa Ikeshiro,  Toshihiro Fujioka,  Nicole R Kilgore,  Carl T Wild,  Graham P Allaway,  Kuo-Hsiung Lee
Affiliations

Affiliation

  • 1 Faculty of Pharmaceutical Sciences, Niigata University of Pharmacy and Applied Life Sciences, Niigata 950-2081, Japan. kasiwada@niigata-pharm.ac.jp
PMID: 15501054 DOI: 10.1016/j.bmcl.2004.09.033
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.

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