LASSBio-1829 Hydrochloride: Development of a New Orally Active N-Acylhydrazone IKK2 Inhibitor with Anti-inflammatory Properties

Inhibitor of nuclear factor κB kinase 2 (IKK2) is suggested to be a potential target for the development of novel anti‐inflammatory and anticancer drugs. In this work, we applied structure‐based drug design to improve the potency of the inhibitor (E)‐N′‐(4‐nitrobenzylidene)‐2‐naphthohydrazide (LASSB...

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Veröffentlicht in:	ChemMedChem 2016-01, Vol.11 (2), p.234-244
Hauptverfasser:	Guedes, Isabella A., Freitas, Rosana H. C. N., Cordeiro, Natália M., Nascimento, Thaís S. do, Valerio, Tayna S., Fernandes, Patrícia D., Dardenne, Laurent E., Fraga, Carlos A. M.
Format:	Artikel
Sprache:	eng
Schlagworte:	Administration, Oral anti-inflammatory agents Anti-Inflammatory Agents, Non-Steroidal - administration & dosage Anti-Inflammatory Agents, Non-Steroidal - chemistry Anti-Inflammatory Agents, Non-Steroidal - pharmacology Benzylidene Compounds - administration & dosage Benzylidene Compounds - chemistry Benzylidene Compounds - pharmacology Dose-Response Relationship, Drug Drug Design Humans I-kappa B Kinase - antagonists & inhibitors I-kappa B Kinase - metabolism IKK2 Models, Molecular molecular docking Molecular Structure N-acylhydrazones Naphthalenes - administration & dosage Naphthalenes - chemistry Naphthalenes - pharmacology Protein Kinase Inhibitors - administration & dosage Protein Kinase Inhibitors - chemistry Protein Kinase Inhibitors - pharmacology Structure-Activity Relationship structure-based drug design
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