e.g. Filippa Pettersson or Cancer Res. 75(6) , 1102-12, (2015) or 10.1002/anie.201600521
Novel and selective imidazole-containing biphenyl inhibitors of protein farnesyltransferase
ML Curtin, AS Florjancic, J Cohen, WZ Gu…
Index: Curtin, Michael L.; Florjancic, Alan S.; Cohen, Jerome; Gu, Wen-Zhen; Frost, David J.; Muchmore, Steven W.; Sham, Hing L. Bioorganic and Medicinal Chemistry Letters, 2003 , vol. 13, # 7 p. 1367 - 1371
A series of imidazole-containing biphenyls was prepared and evaluated in vitro for inhibition of FTase and cellular Ras processing. Several of these analogues, such as 21, are potent inhibitors of FTase (< 1nM), FTase/GGTase selective (> 300-fold) and cellularly active (≤ 80nM). An X-ray crystal structure of inhibitor 21 bound to rat farnesyltransferase is also presented.
