0

Synthesis of Hemslecin A Derivatives: A New Class of Hepatitis B Virus Inhibitors

Rui-Hua Guo, Chang-An Geng, Xiao-Yan Huang, Yun-Bao Ma, Quan Zhang, Li-Jun Wang, Xue-Mei Zhang, Rong-Ping Zhang, Ji-Jun Chen

Bioorg Med Chem Lett. 2013 Mar 1;23(5):1201-5.

PMID: 23385212

Abstract:

A series of hemslecin A derivatives were synthesized and evaluated for their anti-hepatitis B virus (HBV) activities, namely, inhibiting the secretion of hepatitis B surface antigen (HBsAg), hepatitis B e antigen (HBeAg), and HBV DNA replication on HepG 2.2.15 cells. Most of the derivatives showed enhanced anti-HBV activities, of which compounds A1-A7, B5, C and E exhibited significant activities inhibiting HBV DNA replication with IC(50) values of 2.8-11.6 μM, comparable to that of the positive control, tenofovir. Compounds A1-A3, A5, B5, and C displayed low cytotoxicities, which resulted in high SI values of 89.7, 55.6, 77.8, >83.4, >55.8, and >150.5, respectively.

Chemicals Related in the Paper:

Catalog Number Product Name Structure CAS Number Price
AP58546342 Hemslecin A Hemslecin A 58546-34-2 Price
qrcode