2. Academic Validation
  3. Anti-AIDS agents. 31. Synthesis and anti-HIV activity of 4-substituted 3',4'-di-O-(-)-camphanoyl-(+)-cis-khellactone (DCK) thiolactone analogs

Anti-AIDS agents. 31. Synthesis and anti-HIV activity of 4-substituted 3',4'-di-O-(-)-camphanoyl-(+)-cis-khellactone (DCK) thiolactone analogs

  • Bioorg Med Chem Lett. 1998 Jun 16;8(12):1483-6. doi: 10.1016/s0960-894x(98)00254-6.
Z Y Yang 1,  Y Xia,  P Xia,  L M Cosentino,  K H Lee
Affiliations

Affiliation

  • 1 Natural Products Laboratory, School of Pharmacy, University of North Carolina, Chapel Hill 27599, USA.
PMID: 9873374 DOI: 10.1016/s0960-894x(98)00254-6
Abstract

Four DCK-thiolactone analogs (3-6) were synthesized asymmetrically and evaluated for anti-HIV activity against HIV-1 replication in H9 lymphocyte cells. Based on the functionality on the thiolactonecoumarin nucleus, activity was in the order: methyl > H > propyl > benzyl. 4-Methyl-3',4'-di-O-(-)-camphanoyl-(+)-cis-khelthiolactone (4) exhibited extremely potent anti-HIV activity with EC50 and therapeutic index values of 0.00718 microM and > 21,300, respectively.

Figures