Pyrazinoindolone inhibitors of MAPKAP-K2

Autor:	David Joseph, Y.-C. Tseng, Amy Gao, Jiang-Ping Wu, R. Wasti, Daniel R. Goldberg, Ming-Hong Hao, Younggi Choi, Chris Pargellis, Mohammed A. Kashem, Zhaoming Xiong, Derek Cogan, Brian Werneburg, Matthew R. Netherton, Rosemarie Sellati, Ji Wang, Carol A. Torcellini, Josephine Pelletier, Donna Skow, Rodney P. DeLeon, Miller Craig Andrew, Lore Gruenbaum, M. Corson, Neil Moss
Rok vydání:	2007
Předmět:	chemistry.chemical_classification Indoles Molecular Structure Chemistry Organic Chemistry Clinical Biochemistry Intracellular Signaling Peptides and Proteins Pharmaceutical Science Tumor cells Protein Serine-Threonine Kinases Biochemistry In vitro Inhibitory Concentration 50 Structure-Activity Relationship Enzyme Drug Discovery Molecular Medicine Potency Combinatorial Chemistry Techniques Pyrazoles Enzyme Inhibitors Molecular Biology
Zdroj:	Bioorganicmedicinal chemistry letters. 18(3)
ISSN:	1464-3405
Popis:	Optimization of pyrazinoindolone inhibitors of MAPKAP-K2 (MK2) provides a reasonable balance of cellular potency and physicochemical properties. Mechanistic studies support the inhibition of MK2 which is responsible for the sub-micromolar cellular efficacy.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::54d0a1a4789b18d191694f405191d34b https://pubmed.ncbi.nlm.nih.gov/18221871 Zobrazit plný text záznamu Full Text from ScienceDirect