Benzopyrimidodiazepinone inhibitors of TNK2. Issue 4 (15th February 2020)

• Record Type: Journal Article
• Authors: 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.
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 30:Issue 4(2020)
• Publication Date: 2020-02-15
• Subjects: TNK2 -- Kinase inhibitor -- Benzopyrimidodiazepinone; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2020.126948
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: Abstract: 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.