Author/Authors :
Qun Li ، نويسنده , , Tongmei Li، نويسنده , , Keith W. Woods، نويسنده , , Wen-Zhen Gu، نويسنده , , Jerry Cohen، نويسنده , , Vincent S. Stoll، نويسنده , , Tomas Galicia، نويسنده , , Charles Hutchins، نويسنده , , David Frost، نويسنده , , Saul H. Rosenberg، نويسنده , , Hing L. Sham، نويسنده ,
Abstract :
A series of analogs of tipifarnib (1) has been synthesized as inhibitors of FTase by substituting the benzimidazolones and indoles for the 2-quinolone of tipifarnib. The novel benzimidazolones are potent and selective FTase inhibitors (FTIs) with IC50 values of the best compounds close to that of tipifarnib. The current series demonstrate good cellular activity as measured in their inhibiting the Ras processing in NIH-3T3 cells, with compounds 2c and 2f displaying EC50 values of 18 and 22 nM, respectively.
