Protein Information

Name Aurora A
Synonyms serine/threonine kinase 6; AIK; ARK 1; ARK1; AURA; AURKA; AURORA 2; AURORA2…

Compound Information

Name piperazine
CAS piperazine

Reference List

PubMed Abstract RScore(About this table)
16891462 Warner SL, Bashyam S, Vankayalapati H, Bearss DJ, Han H, Mahadevan D, Von Hoff DD, Hurley LH: Identification of a lead small-molecule inhibitor of the Aurora kinases using a structure-assisted, fragment-based approach. Mol Cancer Ther. 2006 Jul;5(7):1764-73.

Based on these computational methods, a new generation of inhibitors derived from quinazoline and pyrimidine-based tricyclic scaffolds were synthesized and evaluated for Aurora A kinase inhibitory activity, which led to the identification of 4-(6,7-dimethoxy-9H-1,3,9-triaza-fluoren-4-yl)-piperazine-1-carbothioic acid [4-(pyrimidin-2-ylsulfamoyl)-phenyl]-amide.
33(0,1,1,3) Details
16152590 Weiderhold KN, Randall-Hlubek DA, Polin LA, Hamel E, Mooberry SL: CB694, a novel antimitotic with antitumor activities. Int J Cancer. 2006 Feb 15;118(4):1032-40.

CB694 caused phosphorylation of Aurora A within 8 hr of treatment, and increases in Aurora A protein levels were coincident with mitotic accumulation.
During the course of a mechanism-based screening program aimed at identifying new antimitotic agents, a novel microtubule depolymerizing piperazine derivative, 1-(5-chloro-2-methoxybenzoyl)-4-(3-chlorophenyl) piperazine, was identified.
1(0,0,0,1) Details