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Benzopyrimidodiazepinone inhibitors of TNK2.
Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2020-01-07 , DOI: 10.1016/j.bmcl.2020.126948 Brian J Groendyke 1 , Chelsea E Powell 1 , Frederic Feru 1 , Thomas W Gero 1 , Zhengnian Li 1 , Hilary Szabo 2 , Kevin Pang 3 , John Feutrill 4 , Bailing Chen 4 , Bin Li 4 , Nathanael S Gray 1 , David A Scott 1
Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2020-01-07 , DOI: 10.1016/j.bmcl.2020.126948 Brian J Groendyke 1 , Chelsea E Powell 1 , Frederic Feru 1 , Thomas W Gero 1 , Zhengnian Li 1 , Hilary Szabo 2 , Kevin Pang 3 , John Feutrill 4 , Bailing Chen 4 , Bin Li 4 , Nathanael S Gray 1 , David A Scott 1
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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.
中文翻译：
TNK2的苯并嘧啶二氮杂庚酮抑制剂。
从有效的选择性化合物XMD8-87开始，开发了一系列TNK2苯并嘧啶基二氮杂酮抑制剂的SAR。引入了一组不同的苯胺，以改善体内PK曲线并最小化醌二亚胺形成的风险。
更新日期：2020-01-07
中文翻译：
TNK2的苯并嘧啶二氮杂庚酮抑制剂。
从有效的选择性化合物XMD8-87开始，开发了一系列TNK2苯并嘧啶基二氮杂酮抑制剂的SAR。引入了一组不同的苯胺，以改善体内PK曲线并最小化醌二亚胺形成的风险。
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