期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 22, 期 20, 页码 6338-6342出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2012.08.086
关键词
MDM2; p53; Dihydroimidazothiazole; Protein-protein interaction inhibitor
Starting with Nutlins as an initial lead, we designed and generated bicyclic scaffolds aiming to place cis-bischlorophenyl moiety at the equivalent location where the hydrophobic interaction with MDM2 could be expected. As a result, we discovered novel MDM2 inhibitors possessing a dihydroimidazothiazole scaffold. Further exploration of the side chains on the dihydroimidazothiazole scaffold aided by molecular modeling resulted in compounds exhibiting almost comparable in vitro potency to Nutlin-3a. (c) 2012 Elsevier Ltd. All rights reserved.
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