Anti-HBV agents. Part 2: synthesis and in vitro anti-hepatitis B virus activities of alisol A derivatives.
Chemical modifications were performed on hydroxyl groups at C-11,23,24,25 positions and C-13(17) double bond of alisol A for structure-activity relationship study. Forty-one derivatives of alisol A were synthesized and assayed for their in vitro anti-hepatitis B virus (HBV) activities and cytotoxicities. Of them, 14 compounds were active against HBV surface antigen (HBsAg) and HBV e antigen (HBeAg) secretion in HepG 2.2.15 cells, and the most promising compound 25 exhibited high activities against secretion of HBsAg (IC(50)=0.028 mM), HBeAg (IC(50)=0.027 mM) and remarkable selective indices (SI(HBsAg) >90, SI(HBeAg) >93).
Zhang
Quan
Q
State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences, Kunming, PR China.
Jiang
Zhi-Yong
ZY
Luo
Jie
J
Liu
Ji-Feng
JF
Ma
Yun-Bao
YB
Guo
Rui-Hua
RH
Zhang
Xue-Mei
XM
Zhou
Jun
J
Chen
Ji-Jun
JJ
D000998:Antiviral Agents / Q000138:chemical synthesis* / Q000378:metabolism / Q000494:pharmacology; D002460:Cell Line; D002626:Chemistry, Pharmaceutical / Q000379:methods; D002783:Cholestenones / Q000138:chemical synthesis* / Q000494:pharmacology; D006514:Hepatitis B Surface Antigens / Q000378:metabolism; D006515:Hepatitis B virus / Q000187:drug effects* / Q000378:metabolism; D006801:Humans
D000998:Antiviral Agents; D002783:Cholestenones; D006514:Hepatitis B Surface Antigens; C000050:alisol A