Design of potent thiophene inhibitors of polo-like kinase 1 with improved solubility and reduced protein binding

A series of thiophene PLK1 inhibitors was optimized for increased solubility and reduced protein binding through the appendage of basic amine functionality. Interesting selectivity between PLK1 and PLK3 was also obtained through these modi. cations. (C) 2009 Published by Elsevier Ltd.