The preparation of ester heterocycles mostly uses heteroatoms as nucleophilic sites, which are achieved by intramolecular substitution or addition reactions. Compound: 4-Aminopyrimidine( cas:591-54-8 ) is researched.Recommanded Product: 591-54-8.Huang, Pan; Le, Xiangyang; Huang, Fei; Yang, Jie; Yang, Haofeng; Ma, Junlong; Hu, Gaoyun; Li, Qianbin; Chen, Zhuo published the article 《Discovery of a Dual Tubulin Polymerization and Cell Division Cycle 20 Homologue Inhibitor via Structural Modification on Apcin》 about this compound( cas:591-54-8 ) in Journal of Medicinal Chemistry. Keywords: anticancer therapeutics Cdc20 inhibitor tubulin polymerization apoptosis PARP. Let’s learn more about this compound (cas:591-54-8).
Apcin is one of the few compounds that have been previously reported as a Cdc20 specific inhibitor, although Cdc20 is a very promising drug target. We reported here the design, synthesis, and biol. evaluations of 2,2,2-trichloro-1-aryl carbamate derivatives as Cdc20 inhibitors. Among these derivatives, compound 9f(I) was much more efficient than the pos. compound apcin in inhibiting cancer cell growth, but it had approx. the same binding affinity with apcin in SPR assays. It is possible that another mechanism of action might exist. Further evidence demonstrated that compound 9f also inhibited tubulin polymerization, disorganized the microtubule network, and blocked the cell cycle at the M phase with changes in the expression of cyclins. Thus, it induced apoptosis through the activation of caspase-3 and PARP. In addition, compound 9f inhibited cell migration and invasion in a concentration-dependent manner. These results provide guidance for developing the current series as potential new anticancer therapeutics.
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