Synthesis and anti-HIV-1 activities of novel podophyllotoxin derivatives

  • Bioorg Med Chem Lett. 2007 Apr 1;17(7):2091-5. doi: 10.1016/j.bmcl.2006.11.070.
Shi-Wu Chen  1 ,  Yun-Hua Wang ,  Yan Jin ,  Xuan Tian ,  Yong-Tang Zheng ,  Du-Qiang Luo ,  Yong-Qiang Tu
Affiliations
  • 1. State Key Laboratory of Applied Organic Chemistry, School of Pharmacy, Lanzhou University, Lanzhou 730000, PR China.
PMID: 17317161 DOI: 10.1016/j.bmcl.2006.11.070
Abstract

In order to explore the range of biological activities of the podophyllotoxin compound class, a novel series of derivatives of podophyllotoxin, which were conjugates containing stavudine and different structural podophyllotoxin analogues, were designed, synthesized, and evaluated for their anti-HIV-1 activities in vitro. Among these compounds, 19d and 19c showed the highest anti-HIV-1 activities with EC(50) values of 0.17 and 0.29 microM and TI values of 466.9 and 354.5, respectively.