Discovery of (R)-5-(benzo[d][1,3]dioxol-5-yl)-7-((1-(vinylsulfonyl)pyrrolidin-2-yl)methyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine (B6) as a potent Bmx inhibitor for the treatment of NSCLC

[Display omitted] Described as a Btk inhibitor, ibrutinib also potently inhibits Bmx and EGFR, two good targets for lung cancer. Owing to its high CLogP (4.07) and low aqueous solubility (

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Bibliographische Detailangaben
Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2017-09, Vol.27 (17), p.4171-4175
Hauptverfasser:	He, Linhong, Li, Da, Zhang, Chufeng, Bai, Peng, Chen, Lijuan
Format:	Artikel
Sprache:	eng
Schlagworte:	Antineoplastic Agents - chemical synthesis Antineoplastic Agents - chemistry Antineoplastic Agents - pharmacology Bmx Carcinoma, Non-Small-Cell Lung - drug therapy Carcinoma, Non-Small-Cell Lung - pathology Cell Line, Tumor Cell Proliferation - drug effects ClogP Dose-Response Relationship, Drug Drug Discovery Drug Screening Assays, Antitumor EGFR Humans Lung Neoplasms - drug therapy Lung Neoplasms - pathology Molecular Conformation NSCLC Protein Kinase Inhibitors - chemical synthesis Protein Kinase Inhibitors - chemistry Protein Kinase Inhibitors - pharmacology Protein-Tyrosine Kinases - antagonists & inhibitors Protein-Tyrosine Kinases - metabolism Solubility Structure-Activity Relationship
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Beschreibung
Zusammenfassung:	[Display omitted] Described as a Btk inhibitor, ibrutinib also potently inhibits Bmx and EGFR, two good targets for lung cancer. Owing to its high CLogP (4.07) and low aqueous solubility (
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2017.07.009