Anti-HBV agents. Part 1: Synthesis of alisol A derivatives: a new class of hepatitis B virus inhibitors.
A series of alisol A derivatives were synthesized and evaluated for their anti-hepatitis B virus (HBV) activities and cytotoxicities in vitro. The preliminary investigation demonstrates that simple modifications of the parent structure of alisol A can produce a number of potentially important derivatives against HBV. The most active anti-HBV compound 6a showed high activities against the secretion of HBV surface antigen (IC(50)=0.024 mM), HBV e antigen (IC(50)=0.028 mM) and remarkable selective indices (SI(HBsAg)>108, SI(HBeAg)>93), which was selected for further evaluation as a novel HBV inhibitor.
Zhang
Quan
Q
State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences, Lanhei Road, Kunming 650204, PR China.
Jiang
Zhi-Yong
ZY
Luo
Jie
J
Cheng
Pi
P
Ma
Yun-Bao
YB
Zhang
Xue-Mei
XM
Zhang
Feng-Xue
FX
Zhou
Jun
J
Chen
Ji-Jun
JJ
D000956:Antigens, Viral / Q000737:chemistry; D000998:Antiviral Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D002783:Cholestenones / Q000138:chemical synthesis* / Q000737:chemistry; D004279:DNA, Viral; D015195:Drug Design; D006509:Hepatitis B / Q000188:drug therapy*; D006511:Hepatitis B Antigens / Q000276:immunology; D006515:Hepatitis B virus / Q000378:metabolism*; D006801:Humans; D017665:Hydroxyl Radical; D020128:Inhibitory Concentration 50; D008956:Models, Chemical; D014779:Virus Replication / Q000187:drug effects
D000956:Antigens, Viral; D000998:Antiviral Agents; D002783:Cholestenones; D004279:DNA, Viral; D006511:Hepatitis B Antigens; C000050:alisol A; D017665:Hydroxyl Radical