The discovery of novel tartrate-based TNF-α converting enzyme (TACE) inhibitors

Synthesis and optimization of novel tartrate TACE inhibitors are described. A novel series of TNF-α convertase (TACE) inhibitors which are non-hydroxamate have been discovered. These compounds are bis-amides of l-tartaric acid (tartrate) and coordinate to the active site zinc in a tridentate manner....

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2010-02, Vol.20 (3), p.1189-1193
Hauptverfasser:	Rosner, Kristin E., Guo, Zhuyan, Orth, Peter, Shipps, Gerald W., Belanger, David B., Chan, Tin Yau, Curran, Patrick J., Dai, Chaoyang, Deng, Yongqi, Girijavallabhan, Vinay M., Hong, Liwu, Lavey, Brian J., Lee, Joe F., Li, Dansu, Liu, Zhidan, Popovici-Muller, Janeta, Ting, Pauline C., Vaccaro, Henry, Wang, Li, Wang, Tong, Yu, Wensheng, Zhou, Guowei, Niu, Xiaoda, Sun, Jing, Kozlowski, Joseph A., Lundell, Daniel J., Madison, Vincent, McKittrick, Brian, Piwinski, John J., Shih, Neng -Yang, Arshad Siddiqui, M., Strickland, Corey O.
Format:	Artikel
Sprache:	eng
Schlagworte:	ADAM Proteins - antagonists & inhibitors ADAM Proteins - metabolism ADAM17 Protein Binding Sites Biological and medical sciences Bones, joints and connective tissue. Antiinflammatory agents Combinatorial Chemistry Techniques Crystallography, X-Ray Drug Discovery - methods Humans Medical sciences Pharmacology. Drug treatments Protease Inhibitors - chemistry Protease Inhibitors - metabolism Protease Inhibitors - pharmacology TACE TACE inhibitors Tartrates Tartrates - chemistry Tartrates - metabolism Tartrates - pharmacology Tumor Necrosis Factor-alpha - metabolism
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