Novel triazole based inhibitors of Ras farnesyl transferase

Ashis K. Saha,Li Liu,Richard Simoneaux,Bart DeCorte,Christophe Meyer,Stacy Skrzat,Henry J. Breslin,Michael J. Kukla,Dave W. End

Bioorganic & Medicinal Chemistry Letters（2006）

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摘要

A novel series of potent inhibitors of Ras farnesyl transferase possessing a 1,2,4-triazole pharmacophore (5) is described. These inhibitors were discovered from a parallel synthesis effort and were subsequently optimized to in vitro IC50 value of less than 1nM (19).

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关键词

Farnesyl transferase,Triazole,Ras,Parallel synthesis

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