Bioorganic and Medicinal Chemistry Letters p. 4732 - 4735 (2011)
Update date:2022-08-02
Topics: Synthesis Biological Evaluation Structure-Activity Relationship N-Substituted Matrinic acid Host heat-stress cognate 70 (Hsc70)
Du, Na-Na
Li, Xin
Wang, Yu-Ping
Liu, Fei
Liu, Yan-Xin
Li, Chun-Xin
Peng, Zong-Gen
Gao, Li-Mei
Jiang, Jian-Dong
Song, Dan-Qing
Oxymatrine (1) is a natural anti-hepatitis B virus (HBV) drug that down-regulates host heat-stress cognate 70 (Hsc70) expression through a mechanism different from that of nucleosides. Taking Hsc70 as a target against HBV, 26 novel N-substituted matrinic acid analogs were designed, synthesized and evaluated for their regulation of Hsc70 mRNA expression with 1 as the lead. The SAR analysis revealed that (i) the carboxyl group at the 11-position was required for activity; (ii) introducing of a substituent on the nitrogen atom at the 12-position of 3, especially substituted benzyl, might significantly improve the activity. Among these analogs, compound 9p possessing N-p-methoxylbenzyl afforded an increased anti-HBV effect in comparison with 1. We consider 9p a promising anti-HBV candidate.
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