Design, Synthesis, and Pharmacological Evaluation of Novel Multisubstituted Pyridin-3-amine Derivatives as Multitargeted Protein Kinase Inhibitors for the Treatment of Non-Small Cell Lung Cancer

A novel series of pyridin-3-amine derivatives were designed, synthesized, and evaluated as multitargeted protein kinase inhibitors for the treatment of non-small cell lung cancer (NSCLC). Hit 1 was first disclosed by in silico screening against fibroblast growth factor receptors (FGFR), which was su...

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Veröffentlicht in:	Journal of medicinal chemistry 2017-07, Vol.60 (14), p.6018-6035
Hauptverfasser:	Zhu, Wei, Chen, Hui, Wang, Yulan, Wang, Jiang, Peng, Xia, Chen, Xianjie, Gao, Yinglei, Li, Chunpu, He, Yulong, Ai, Jing, Geng, Meiyu, Zheng, Mingyue, Liu, Hong
Format:	Artikel
Sprache:	eng
Schlagworte:	Aminopyridines - chemical synthesis Aminopyridines - pharmacokinetics Aminopyridines - pharmacology Animals Antineoplastic Agents - chemical synthesis Antineoplastic Agents - pharmacokinetics Antineoplastic Agents - pharmacology Carcinoma, Non-Small-Cell Lung - drug therapy Cell Line, Tumor Cell Proliferation - drug effects Databases, Chemical Drug Design Drug Screening Assays, Antitumor Female Heterografts Humans Indazoles - chemical synthesis Indazoles - pharmacokinetics Indazoles - pharmacology Lung Neoplasms - drug therapy Mice Mice, Nude Molecular Docking Simulation Neoplasm Transplantation Phosphorylation Protein Kinase Inhibitors - chemical synthesis Protein Kinase Inhibitors - pharmacokinetics Protein Kinase Inhibitors - pharmacology Protein-Tyrosine Kinases - antagonists & inhibitors Protein-Tyrosine Kinases - metabolism Pyridines - chemical synthesis Pyridines - pharmacokinetics Pyridines - pharmacology Rats, Sprague-Dawley Signal Transduction Stereoisomerism Structure-Activity Relationship
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