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2-Arylindole-3-acetamides: FPP-competitive inhibitors of farnesyl protein transferase |
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| Authors: | Trotter B W Quigley A G Lumma W C Sisko J T Walsh E S Hamann C S Robinson R G Bhimnathwala H Kolodin D G Zheng W Buser C A Huber H E Lobell R B Kohl N E Williams T M Graham S L Dinsmore C J |
| Affiliation: | Department of Medicinal Chemistry, Merck Research Laboratories, West Point, PA 19486, USA. bwesley_trotter@merck.com |
| Abstract: |  A series of 2-arylindole-3-acetamide farnesyl protein transferase inhibitors has been identified. The compounds inhibit the enzyme in a farnesyl pyrophosphate-competitive manner and are selective for farnesyl protein transferase over the related enzyme geranylgeranyltransferase-I. A representative member of this series of inhibitors demonstrates equal effectiveness against HDJ-2 and K-Ras farnesylation in a cell-based assay when geranylgeranylation is suppressed. |
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