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Novel triazole based inhibitors of Ras farnesyl transferase |
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| Authors: | Saha Ashis K Liu Li Simoneaux Richard DeCorte Bart Meyer Christophe Skrzat Stacy Breslin Henry J Kukla Michael J End Dave W |
| Affiliation: | aDepartment of Medicinal Chemistry, Janssen Research Foundation, Johnson & Johnson Pharmaceutical Research & Development, Welsh and McKean Roads, Spring House, PA 19477, USA bDepartment of Computational Chemistry, Johnson & Johnson Pharmaceutical Research & Development, Val de Reuil, France cDepartment of Oncology, Janssen Research Foundation, Johnson & Johnson Pharmaceutical Research & Development, Welsh and McKean Roads, Spring House, PA 19477, USA |
| Abstract: |  A novel series of potent inhibitors of Ras farnesyl transferase possessing a 1,2,4-triazole pharmacophore is described. These inhibitors were discovered from a parallel synthesis effort and were subsequently optimized to in vitro IC50 value of less than 1 nM. |
| Keywords: | Farnesyl transferase Triazole Ras Parallel synthesis |
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