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

Emmitte Kyle A,Adjabeng George M, Adjebang George M,Andrews C Webb,Alberti Jennifer G Badiang,Bambal Ramesh,Chamberlain Stanley D,Davis-Ward Ronda G,Dickson Hamilton D,Hassler Daniel F,Hornberger Keith R,Jackson Jeffrey R,Kuntz Kevin W,Lansing Timothy J,Mook Robert A,Nailor Kristen E,Pobanz Mark A,Smith Stephon C, Sung Chiu-Mei,Cheung Mui

Bioorganic & Medicinal Chemistry Letters（2009）

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摘要

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 modifications.

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关键词

Polo-like kinase,Anti-mitotic,Cell cycle inhibitor,Thiophene,Solubility,Protein binding

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