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Oxo-piperazine derivatives of N-arylpiperazinones as inhibitors of farnesyltransferase |
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| Authors: | Dinsmore C J Bergman J M Wei D D Zartman C B Davide J P Greenberg I B Liu D O'Neill T J Gibbs J B Koblan K S Kohl N E Lobell R B Chen I W McLoughlin D A Olah T V Graham S L Hartman G D Williams T M |
| Affiliation: | Department of Medicinal Chemistry, Merck Research Laboratories, West Point, PA 19486, USA. christopher_dinsmore@merck.com |
| Abstract: | The evaluation of SAR associated with the insertion of carbonyl groups at various positions of N-arylpiperazinone farnesyltransferase inhibitors is described herein. 1-Aryl-2,3-diketopiperazine derivatives exhibited the best balance of potency and pharmacokinetic profile relative to the parent 1-aryl-2-piperazinones. |
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