769949-52-2Relevant academic research and scientific papers
Synthesis of A/B ring analogs of territrem B and evaluation of their biological activities
Zhao, Jinhao,Zhao, Feng,Wang, Yanguang,Li, Haibo,Zhang, Qijun,Guenard, Daniel,Ge, Qiufu,Wei, Erqing,Jiang, Hao,Wu, Yihang,Wang, Lin,Jiang, Hualiang,Gueritte, Francoise,Wu, Xiumei,Cheng, Christopher H. K.,Lee, Shoei-Sheng,Zhao, Yu
, p. 1832 - 1853 (2007/10/03)
Two series of territrem B analogs, i.e., 5-10, containing both the 2-en-1-one-A-ring and the aromatic-E-ring pharmacophores were designed and synthesized from jujubogenin (4a). The anti-acetylcholinesterase (anti-AChE), anti-caspase-3, and other biological activities of these territrem-B analogs and their intermediates were assessed. Compound 9b, 22a, and 24f were shown to be weak inhibitors of AChE. None of the synthesized compounds exhibited significant inhibitory activity on caspase-3. On the other hand, compounds 22e, 24a, 7b, and 8a showed mild cytotoxicity on cultured KB cells, with IC50 values of 2.0, 3.5, 6.5, and 14 μM, respectively. In addition, compounds 23b and 5f were active against injury arising from oxygen-glucose deprivation.
