Synthesis and anti-HIV-1 activities of novel podophyllotoxin derivatives.
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.
Chen
Shi-Wu
SW
State Key Laboratory of Applied Organic Chemistry, School of Pharmacy, Lanzhou University, Lanzhou 730000, PR China.
Wang
Yun-Hua
YH
Jin
Yan
Y
Tian
Xuan
X
Zheng
Yong-Tang
YT
Luo
Du-Qiang
DQ
Tu
Yong-Qiang
YQ
D019380:Anti-HIV Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D000972:Antineoplastic Agents, Phytogenic / Q000138:chemical synthesis / Q000494:pharmacology*; D002460:Cell Line; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D015195:Drug Design; D015658:HIV Infections / Q000188:drug therapy*; D015497:HIV-1 / Q000378:metabolism; D006801:Humans; D020128:Inhibitory Concentration 50; D009682:Magnetic Resonance Spectroscopy; D008956:Models, Chemical; D008968:Molecular Conformation; D011034:Podophyllotoxin / Q000031:analogs & derivatives* / Q000138:chemical synthesis*; D013055:Spectrophotometry, Infrared; D018119:Stavudine / Q000737:chemistry / Q000494:pharmacology*
D019380:Anti-HIV Agents; D000972:Antineoplastic Agents, Phytogenic; D018119:Stavudine; D011034:Podophyllotoxin