Anti-AIDS agents. Part 58: synthesis and anti-HIV activity of 1-thia-di-O-(-)-camphanoyl-(+)-cis-khellactone (1-thia-DCK) analogues

  • Bioorg Med Chem Lett. 2004 Jun 21;14(12):3341-3. doi: 10.1016/j.bmcl.2004.03.051.
Peng Xia  1 ,  Zhi-Jian Yin ,  Ying Chen ,  Qian Zhang ,  Beina Zhang ,  Yi Xia ,  Zheng-Yu Yang ,  Nicole Kilgore ,  Carl Wild ,  Susan L Morris-Natschke ,  Kuo-Hsiung Lee
Affiliations
  • 1. Department of Medicinal Chemistry, School of Pharmacy, Fudan University, Shanghai 200032, China. [email protected]
PMID: 15149703 DOI: 10.1016/j.bmcl.2004.03.051
Abstract

Two 1-thia-DCK analogues (9a and 9b) were synthesized and evaluated for inhibition of HIV-1 replication in H9 lymphocytes. Compound 9a showed excellent anti-HIV activity with an EC(50) value of 0.00012 microM and therapeutic index of 1408000. Compound 9b was less active with EC(50) and TI values of 3.11 microM and 62.3, respectively. The bioassay results indicated that thia-DCK analogues merit attention as potential HIV-1 inhibitors.