950-82-3Relevant academic research and scientific papers
Design and Synthesis of Cajanine Analogues against Hepatitis C Virus through Down-Regulating Host Chondroitin Sulfate N-Acetylgalactosaminyltransferase 1
Ji, Xing-Yue,Chen, Jin-Hua,Zheng, Guang-Hui,Huang, Meng-Hao,Zhang, Lei,Yi, Hong,Jin, Jie,Jiang, Jian-Dong,Peng, Zong-Gen,Li, Zhuo-Rong
, p. 10268 - 10284 (2016/12/07)
There still remains a need to develop new anti-HCV agents with distinct mechanism of action (MOA) due to the occurrence of resistance to direct-acting antiviral agents (DAAs). Cajanine, a stilbenic component isolated from Cajanus cajan L., was identified as a potent HCV inhibitor by phenotypic screening in this work (EC50 = 3.17 ± 0.75 μM). The intensive structure optimization provided significant insights into the structure-activity relationships. Furthermore, the MOA study revealed that cajanine inhibited HCV replications via down-regulating a cellular protein chondroitin sulfate N-acetylgalactosaminyltransferase 1. In consistency with this host-targeting mechanism, cajanine showed the similar magnitude of inhibitory activity against both drug-resistant and wild-type HCV and synergistically inhibited HCV replication with approved DAAs. Taken together, our study not only presented cajanine derivatives as a novel class of anti-HCV agents but also discovered a promising anti-HCV target to combat drug resistance.
A general approach for the synthesis of phenolic natural products. Facile syntheses of grifolin and colletochlorins B and D
Saimoto,Ueda,Sashiwa,Shigemasa,Hiyama
, p. 1178 - 1185 (2007/10/02)
A general approach is established for the synthesis of phenolic compounds having terpenoid side chains: (1) protection of the phenolic hydroxyls in the aromatic precursor by ether formation, (2) coupling the aromatic part with a terpenoid bromide, and (3) deprotection to regenerate the hydroxyl groups. This strategy was successfully applied to the synthesis of colletochlorins B and D and grifolin. Some of the colletochlorin derivatives were found to inhibit the cell growth of P388.
