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Macrocyclic piperazinones as potent dual inhibitors of farnesyltransferase and geranylgeranyltransferase-I |
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| Authors: | Dinsmore Christopher J Zartman C Blair Bergman Jeffrey M Abrams Marc T Buser Carolyn A Culberson J Christopher Davide Joseph P Ellis-Hutchings Michelle Fernandes Christine Graham Samuel L Hartman George D Huber Hans E Lobell Robert B Mosser Scott D Robinson Ronald G Williams Theresa M |
| Institution: | Department of Medicinal Chemistry, Merck Research Laboratories, West Point, PA 19486, USA. christopher_dinsmore@merck.com |
| Abstract: | A series of macrocyclic piperazinone compounds with dual farnesyltransferase/geranylgeranyltransferase-I inhibitory activity was prepared. These compounds were found to be potent inhibitors of protein prenylation in cell culture. A hypothesis for the binding mode of compound 3o in FPTase is proposed. |
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