Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10594210 | Bioorganic & Medicinal Chemistry Letters | 2012 | 5 Pages |
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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Authors
Adrian Wai-Hing Cheung, Bruce Banner, Jolly Bose, Kyungjin Kim, Shiming Li, Nicholas Marcopulos, Lucja Orzechowski, Joseph A. Sergi, Kshitij C. Thakkar, Bing-Bing Wang, Weiya Yun, Catherine Zwingelstein, Steven Berthel, Andrée R. Olivier,