Benzopyrimidodiazepinone inhibitors of TNK2

[Display omitted] The SAR of a series of benzopyrimidodiazepinone inhibitors of TNK2 was developed, starting from the potent and selective compound XMD8-87. A diverse set of anilines was introduced in an effort to improve the in vivo PK profile and minimize the risk of quinone diimine formation.

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2020-02, Vol.30 (4), p.126948, Article 126948
Hauptverfasser:	Groendyke, Brian J., Powell, Chelsea E., Feru, Frederic, Gero, Thomas W., Li, Zhengnian, Szabo, Hilary, Pang, Kevin, Feutrill, John, Chen, Bailing, Li, Bin, Gray, Nathanael S., Scott, David A.
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Azepines - chemistry Azepines - metabolism Azepines - pharmacokinetics Benzopyrimidodiazepinone Cell Line, Tumor Chemistry Chemistry, Medicinal Chemistry, Organic Half-Life Humans Inhibitory Concentration 50 Kinase inhibitor Life Sciences & Biomedicine Mice Microsomes, Liver - metabolism Pharmacology & Pharmacy Physical Sciences Protein Binding Protein Kinase Inhibitors - chemistry Protein Kinase Inhibitors - metabolism Protein Kinase Inhibitors - pharmacokinetics Protein-Tyrosine Kinases - antagonists & inhibitors Protein-Tyrosine Kinases - genetics Protein-Tyrosine Kinases - metabolism Science & Technology Structure-Activity Relationship TNK2
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Zusammenfassung:	[Display omitted] The SAR of a series of benzopyrimidodiazepinone inhibitors of TNK2 was developed, starting from the potent and selective compound XMD8-87. A diverse set of anilines was introduced in an effort to improve the in vivo PK profile and minimize the risk of quinone diimine formation.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2020.126948