Tubulin, the major protein component of microtubules, is the target of numerous antimitotic drugs. A large number of structurally diverse antimitotic agents have been identified as inhibitors of the tubulin polymerization. HU Youhong’s group and LOU Liguang’s group of Shanghai Institute of Materia Medica(SIMM), CAS, discover a new class of tubulin polymerization inhibitors.

A novel series of 2,4,5-substituted pyrimidines were observed to be an excellent inhibitor of tubulin polymerization and to display significantly high antiproliferative activities against several cancer cell lines. These compounds displayed a high propensity to arrests cells at the G2/M phase of the cell cycle.
The observations demonstrate that 2,4,5-substituted pyrimidines represent a new class of tubulin polymerization inhibitors with significant antiproliferative activity. Additional research on the mechanisms and SARs of these compounds is under progress.

This work was supported by National Natural Science Foundation of China, Major Projects in National Ministry of Science and Technology, Shanghai Commission of Science and Technology. This work has been published on Journal of Medicinal Chemistry (2011, 54, 2127-2142) .

Full text: http://pubs.acs.org/doi/full/10.1021/jm101388d