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Fused bi-heteroaryl substituted hydantoin compounds as TACE inhibitors. | LitMetric
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Fused bi-heteroaryl substituted hydantoin compounds as TACE inhibitors.

Ling Tong Seong Heon Kim Kristin Rosner Wensheng Yu Bandarpalle B Shankar Lei Chen Dansu Li Chaoyang Dai Vinay Girijavallabhan Janeta Popovici-Muller Liping Yang Guowei Zhou Aneta Kosinski M Arshad Siddiqui Neng-Yang Shih Zhuyan Guo Peter Orth Shiying Chen Daniel Lundell Xiaoda Niu

Bioorg Med Chem Lett

Department of Discovery Chemistry, Merck & Co., Inc., 2000 Galloping Hill Road, Kenilworth, NJ 07033, USA; Department of Chemistry, Modeling and Informatics, Merck & Co., Inc., 2000 Galloping Hill Road, Kenilworth, NJ 07033, USA; Department of Pharmacokinetics, Merck & Co., Inc., 2000 Galloping Hill Road, Kenilworth, NJ 07033, USA; Department of Immunology, Merck & Co., Inc., 2000 Galloping Hill Road, Kenilworth, NJ 07033, USA.

Published: July 2017

We have identified a series of hydantoin-derived TNF-a converting enzyme (TACE) inhibitors containing a pendant fused bi-heteroaryl group, which demonstrate sub-nanomolar potency (Ki), excellent activity in human whole blood assay, and improved DMPK profiles over prior series.

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 Source
http://dx.doi.org/10.1016/j.bmcl.2017.05.062DOI Listing

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