Anti-AIDS agents part 41: synthesis and anti-HIV activity of 3',4'-di-o-(-)-camphanoyl-(+)-cis-khellactone (DCK) lactam analogues.
DCK lactam analogues were synthesized and evaluated for anti-HIV activity against HIV-1 replication in H9 lymphocyte cells. 4-Methyl-DCK lactam (11a) exhibited potent anti-HIV activity with EC50 and therapeutic index values of 0.00024 microM and 119,333, respectively.
Yang
Z Y
ZY
Natural Products Laboratory, School of Pharmacy, University of North Carolina, Chapel Hill 27599, USA.
Xia
Y
Y
Xia
P
P
Brossi
A
A
Cosentino
L M
LM
Lee
K H
KH
D019380:Anti-HIV Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D001671:Biochemistry / Q000379:methods; D019086:Bridged Bicyclo Compounds, Heterocyclic / Q000737:chemistry* / Q000494:pharmacology*; D002164:Camphor / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology; D003374:Coumarins / Q000737:chemistry* / Q000494:pharmacology*; D004353:Drug Evaluation, Preclinical / Q000379:methods; D006801:Humans; D007769:Lactams / Q000737:chemistry; D008214:Lymphocytes / Q000187:drug effects / Q000821:virology; D015363:Quinolones / Q000138:chemical synthesis* / Q000494:pharmacology*; D013329:Structure-Activity Relationship
C120314:3',4'-di-O-camphanoyl-4-methylkhellactone; C413722:3',4'-di-O-camphanoyl-4-methylkhellactone lactam; D019380:Anti-HIV Agents; D019086:Bridged Bicyclo Compounds, Heterocyclic; D003374:Coumarins; D007769:Lactams; D015363:Quinolones; D002164:Camphor