Synthesisandanti-HIV-1activitiesofnovelpodophyllotoxinderivatives.docVIP

Bioorganic Medicinal Chemistry LettersVolume 17, Issue 7, 1 April 2007, Pages 2091-2095 Synthesis and anti-HIV-1 activities of novel podophyllotoxin derivatives References and further reading may be available for this article. To view references and further reading you must purchase this article. Shi-Wu Chena, c, Yun-Hua Wangb, d, Yan Jina, Xuan Tiana, , , Yong-Tang Zhengb, , Du-Qiang Luob and Yong-Qiang Tua, aState Key Laboratory of Applied Organic Chemistry, Lanzhou University, Lanzhou 730000, PR China bLaboratory of Molecular Immunopharmacology, Kunming Institute of Zoology, Chinese Academy of Sciences, Kunming 650223, PR China cSchool of Pharmacy, Lanzhou University, Lanzhou 730000, PR China dGraduate School of Chinese Academy of Sciences, Beijing 100039, PR China Received 2 September 2006;? revised 13 October 2006;? accepted 7 November 2006.? Available online 1 December 2006. 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 EC50 values of 0.17 and 0.29?μM and TI values of 466.9 and 354.5, respectively. Graphical abstract A novel series of derivatives of podophyllotoxin as anti-HIV-1 agents were synthesized, 19d and 19c showed the highest anti-HIV activity with EC50 values of 0.17 and 0.29?μM and TI values of 466.9 and 354.5, respectively. Keywords: Podophyllotoxin; d4T; Anti-HIV; Totoxicity Article Outline Acknowledgements Supplementary data References