Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 16, Issue 12, Pages 3310-3314Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2006.03.055
Keywords
HDM2; p53; protein-protein interaction; HDM2 antagonist; pharmacokinetic; structure-based drug design
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Guided by structure-based drug design, modification of the 1,4-benzodiazepin-2,5-dione lead compound 1 resulted in the discovery of 19, a potent and orally bioavailable antagonist of the HDM2-p53 protein-protein interaction (FP IC50 = 0.7 mu M, F approximate to 100%). (c) 2006 Elsevier Ltd. All rights reserved.
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