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Monocyclic thiophenes as protein tyrosine phosphatase 1B inhibitors: Capturing interactions with Asp48

2006; Elsevier BV; Volume: 16; Issue: 18 Linguagem: Inglês

10.1016/j.bmcl.2006.06.051

1464-3405

Zhao‐Kui Wan, Jinbo Lee, Weixin Xu, David V. Erbe, Diane Joseph‐McCarthy, Bruce Follows, Yanling Zhang,

Bioactive Compounds and Antitumor Agents

A series of monocyclic thiophenes was designed and synthesized as PTP1B inhibitors. Guided by X-ray co-crystal structural information and computational modeling, rational design led to key interactions with Asp48 and improved inhibitory potency against PTP1B.