Synthesis and anti-HBV activity evaluation of Matijin-Su derivatives with aromatic heterocycles
10.11665/j.issn.1000-5048.20150601
- VernacularTitle:含芳杂环取代的马蹄金素衍生物的设计、合成及抗乙肝病毒活性
- Author:
Jingying QIU
1
;
Zhanxing HU
;
Bixue XU
;
Weidong PAN
;
Zhengming HUANG
;
Changxiao LIU
;
Guangyi LIANG
Author Information
1. 徐州医学院,江苏省新药研究与临床药学重点实验室
- Publication Type:Journal Article
- Keywords:
Matijin-Su;
aromatic heterocycles;
synthesis;
anti-HBV activity
- From:
Journal of China Pharmaceutical University
2015;46(6):641-646
- CountryChina
- Language:Chinese
-
Abstract:
Hepatitis B virus(HBV)-infected hepatitis is one of the most common infectious disease worldwide. To find novel effective anti-HBV agents, a series of Matijin-Su(MTS)derivatives with aromatic heterocycles were synthesized and evaluated for their anti- HBV activities in HepG2 2. 2. 15 cells. Among them, compounds 7a(IC50=2. 94 μmol/L)and 9a(IC50=2. 21 μmol/L)exhibited more potent inhibitory activity against the replication of HBV DNA in HepG2 2. 2. 15 cells than that of lead compound MTS(IC50=11. 16 μmol/L). Notably, both 7a and 9a displayed a high selective index(SI)of 146. 39 and > 250, respectively, which were also much higher than that of MTS(SI=10. 78). Therefore, compounds 7a and 9a may be promising anti-HBV agents with safety profile for HBV infection.