3,28-Di-O-(dimethylsuccinyl)-betulin isomers as anti-HIV agents.
Four isomers of 3,28-di-O-(dimethylsuccinyl)-betulin were prepared and evaluated for anti-HIV activity against HIV-1 replication in H9 lymphocyte cells. 3-O-(3',3'-Dimethylsuccinyl)-28-O-(2", 2"-dimethvlsuccinyl)-betulin (11) was the most potent anti-HIV compound with an EC5, value of 0.00087 microM and a TI value of 42,400.
Kashiwada
Y
Y
Niigata College of Pharmacy, Japan. kasiwada@niigata-pharm.ac.jp
Chiyo
J
J
Ikeshiro
Y
Y
Nagao
T
T
Okabe
H
H
Cosentino
L M
LM
Fowke
K
K
Lee
K H
KH
D019380:Anti-HIV Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D002455:Cell Division / Q000187:drug effects; D002460:Cell Line; D020650:Combinatorial Chemistry Techniques; D015497:HIV-1 / Q000187:drug effects / Q000254:growth & development; D006801:Humans; D020128:Inhibitory Concentration 50; D007536:Isomerism; D008214:Lymphocytes / Q000821:virology; D013329:Structure-Activity Relationship; D019802:Succinic Acid / Q000737:chemistry; D013810:Therapeutic Equivalency; D014315:Triterpenes / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D000094062:Betulinic Acid
D019380:Anti-HIV Agents; D019802:Succinic Acid; D014315:Triterpenes; C002503:betulin; D000094062:Betulinic Acid