Xie, Fuchun; Zhao, Hongbing; Li, Dewen; Chen, Hong; Quan, Haitian; Shi, Xiaojing; Lou, Liguang; Hu, Youhong published the artcile< Synthesis and Biological Evaluation of 2,4,5-Substituted Pyrimidines as a New Class of Tubulin Polymerization Inhibitors>, Product Details of C11H17BN2O2, the main research area is pyrimidine derivative preparation SAR tubulin polymerization inhibitor antiproliferative activity.
Members of a series of 2,4,5-substituted pyrimidine derivatives were synthesized, and their interactions with tubulin and their antiproliferative activities against the human hepatocellular carcinoma cells of liver (BEL-7402) were evaluated. One member of this family, the indole-pyrimidine I, having an indole-aryl-substituted aminopyrimidine structure, was observed to be an excellent inhibitor of tubulin polymerization (IC50 = 0.79 μM) and to display significantly high antiproliferative activities against several cancer cell lines with IC50 values ranging from 16 to 62 nM. This substance displayed a high propensity to arrests cells at the G2/M phase of the cell cycle (EC50 = 20 nM). In addition, I was found to competitively inhibit colchicine binding to tubulin, indicating that it binds to the colchicine-binding site of tubulin. The observations made in this investigation demonstrate that 2,4,5-substituted pyrimidines represent a new class of tubulin polymerization inhibitors with significant antiproliferative activity.
Journal of Medicinal Chemistry published new progress about Antimitotic agents. 229009-40-9 belongs to class piperazines, and the molecular formula is C11H17BN2O2, Product Details of C11H17BN2O2.
Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics