2-Amino-7-substituted benzoxazole analogs as potent RSK2 inhibitors

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• 作者：Abran Costales ; Michelle Mathur ; Savithri Ramurthy ; Jiong Lan ; Sharadha Subramanian ; Rama Jain ; Gordana Atallah ; Lina Setti ; Mika Lindvall ; Brent A. Appleton ; Elizabeth Ornelas ; Paul Feucht ; Bob Warne ; Laura Doyle ; Stephen E. Basham ; Ida Aronchik ; Anne B. Jefferson ; Cynthia M. Shafer ; ^{cynthia.shafer@novartis.com" class="auth_mail}
• 关键词：RSK ; Kinase ; Heterocycle ; Benzoxazole ; HTS
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：15 March, 2014
• 年：2014
• 卷：24
• 期：6
• 页码：1592-1596
• 全文大小：2582 K

文摘

2-Amino-7-substituted benzoxazole analogs were identified by HTS as inhibitors of RSK2. Molecular modeling and medicinal chemistry techniques were employed to explore the SAR for this series with a focus of improving in vitro and target modulation potency and physicochemical properties.