306280-20-6Relevant articles and documents
Synthesis, biological evaluation and molecular docking studies of flavone and isoflavone derivatives as a novel class of KSP (kinesin spindle protein) inhibitors
Dong, Jing-Jun,Li, Qing-Shan,Liu, Zhi-Peng,Wang, Shu-Fu,Zhao, Meng-Yue,Yang, Yong-Hua,Wang, Xiao-Ming,Zhu, Hai-Liang
, p. 427 - 433 (2013)
The kinesin spindle protein (KSP) is involved in the formation of bipolar mitotic spindle during cell division and it becomes a new target to overcome the neurotoxicity of MTs inhibitors. A series of flavone and isoflavone derivatives (1a-7c) have been designed, synthesized and evaluated as potential KSP inhibitors. Among them, 2c displayed the most potent inhibitory activity in vitro, which inhibited the growth of MCF-7 and Hela cell lines with IC 50 values of 4.8 and 4.3 μM, respectively, and also exhibited significant KSP inhibitory activity (IC50 = 0.023 μM). The new compounds can induce irregular monoastral spindles, the characteristic phenotype for KSP inhibiting agents. Docking simulation was further performed to determine the probable binding model.