Discovery and preliminary structure–activity relationship studies of novel benzotriazine based compounds as Src inhibitors

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• 作者：Glenn Noronha ; Kathy Barrett ; Jianguo Cao ; Elena Dneprovskaia ; Richard Fine ; Xianchang Gong ; Colleen Gritzen ; John Hood ; Xinshan Kang ; Boris Klebansky et al.
• 关键词：Src inhibitor ; Cancer ; Kinase inhibitor ; Benzotriazines
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2006
• 出版时间：1 November 2006
• 年：2006
• 卷：16
• 期：21
• 页码：5546-5550
• 全文大小：171 K

文摘

We report the discovery and preliminary SAR studies of a series of structurally novel benzotriazine core based small molecules as inhibitors of Src kinase. To the best of our knowledge, benzotriazine template based compounds have not been reported as kinase inhibitors. The 3-(2-(1-pyrrolidinyl)ethoxy)phenyl analogue (43) was identified as one of the most potent inhibitors of Src kinase.