Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10587899 | Bioorganic & Medicinal Chemistry Letters | 2013 | 5 Pages |
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 IC50 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.
Keywords
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
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,