Anti-AIDS agents part 41: synthesis and anti-HIV activity of 3',4'-di-o-(-)-camphanoyl-(+)-cis-khellactone (DCK) lactam analogues

Bioorg Med Chem Lett. 2000 May 15;10(10):1003-5. doi: 10.1016/s0960-894x(00)00126-8.

Abstract

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.

Publication types

  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Anti-HIV Agents / chemical synthesis*
  • Anti-HIV Agents / pharmacology*
  • Biochemistry / methods
  • Bridged Bicyclo Compounds, Heterocyclic / chemistry*
  • Bridged Bicyclo Compounds, Heterocyclic / pharmacology*
  • Camphor / analogs & derivatives*
  • Camphor / chemical synthesis
  • Camphor / pharmacology
  • Coumarins / chemistry*
  • Coumarins / pharmacology*
  • Drug Evaluation, Preclinical / methods
  • Humans
  • Lactams / chemistry
  • Lymphocytes / drug effects
  • Lymphocytes / virology
  • Quinolones / chemical synthesis*
  • Quinolones / pharmacology*
  • Structure-Activity Relationship

Substances

  • 3',4'-di-O-camphanoyl-4-methylkhellactone
  • 3',4'-di-O-camphanoyl-4-methylkhellactone lactam
  • Anti-HIV Agents
  • Bridged Bicyclo Compounds, Heterocyclic
  • Coumarins
  • Lactams
  • Quinolones
  • Camphor