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  • Title: Discovery of novel dihydroimidazothiazole derivatives as p53-MDM2 protein-protein interaction inhibitors: synthesis, biological evaluation and structure-activity relationships.
    Author: Miyazaki M, Kawato H, Naito H, Ikeda M, Miyazaki M, Kitagawa M, Seki T, Fukutake S, Aonuma M, Soga T.
    Journal: Bioorg Med Chem Lett; 2012 Oct 15; 22(20):6338-42. PubMed ID: 22995624.
    Abstract:
    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.
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