1594439-46-9Relevant academic research and scientific papers
Identification of novel bivalent mimetics of annonaceous acetogenins via a scaffold-hopping strategy
Liu, Yanghan,Liu, Yongqiang,Li, Zhen,Zhou, Guang-Biao,Yao, Zhu-Jun,Jiang, Sheng
supporting information, p. 1650 - 1653 (2014/04/17)
A series of novel bivalent mimetics of annonaceous acetogenins have been designed, synthesized, and evaluated. Among these, compound 7 bearing a homopiperazine ring in the middle region exhibited more potent growth inhibitory activity and higher selectivity against cancer cells over normal cells by comparison with AA005. This work indicates that modification of the middle piperazine ring is a useful optimizing tool for the simplified acetogenin mimetics.
Biological evaluation of new mimetics of annonaceous acetogenins: Alteration of right scaffold by click linkage with aromatic functionalities
Liu, Yanghan,Xiao, Qicai,Liu, Yongqiang,Li, Zheng,Qiu, Yatao,Zhou, Guang-Biao,Yao, Zhu-Jun,Jiang, Sheng
, p. 248 - 258 (2014/04/17)
A small library of analogues of annonaceous acetogenins through click linkage with aromatic moieties is established using a convergent modular fragment-assembly approach. These analogues exhibited low micromolar inhibitory activities against the proliferation of several human cancer cell lines. Structure-activity relationship (SAR) of these analogues indicates that replacement of the methoxy groups of ubiquinone ring with methyl groups is proved to be a useful strategy for improving the anticancer activity of quinone-acetogenin hybrids.
