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Novel and selective imidazole-containing biphenyl inhibitors of protein farnesyltransferase
Authors:Curtin Michael L  Florjancic Alan S  Cohen Jerome  Gu Wen-Zhen  Frost David J  Muchmore Steven W  Sham Hing L
Affiliation:Department of Cancer Research, Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, IL 60064, USA. mike.curtin@abbott.com
Abstract: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 (
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