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  • Title: 7-Phenyl-pyrido[2,3-d]pyrimidine-2,4-diamines: novel and highly selective protein tyrosine phosphatase 1B inhibitors.
    Author: Cheung AW, Banner B, Bose J, Kim K, Li S, Marcopulos N, Orzechowski L, Sergi JA, Thakkar KC, Wang BB, Yun W, Zwingelstein C, Berthel S, Olivier AR.
    Journal: Bioorg Med Chem Lett; 2012 Dec 15; 22(24):7518-22. PubMed ID: 23122867.
    Abstract:
    High throughput screening of the Roche compound collection led to the identification of diaminopyrroloquinazoline series as a novel class of PTP1B inhibitors. Structural modification of diaminopyrroloquinazoline series resulted in pyrido[2,3-d]pyrimidine-2,4-diamine series which was further optimized to give compounds 5 and 24 as potent, selective (except T-cell phosphatase) PTP1B inhibitors with good mouse PK properties.
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