作为强效RSK2抑制剂的2-氨基-7-取代苯并恶唑类似物
2-Amino-7-substituted benzoxazole analogs as potent RSK2 inhibitors.
作者信息
Costales Abran, Mathur Michelle, Ramurthy Savithri, Lan Jiong, Subramanian Sharadha, Jain Rama, Atallah Gordana, Setti Lina, Lindvall Mika, Appleton Brent A, Ornelas Elizabeth, Feucht Paul, Warne Bob, Doyle Laura, Basham Stephen E, Aronchik Ida, Jefferson Anne B, Shafer Cynthia M
机构信息
Global Discovery Chemistry/Oncology & Exploratory Chemistry, Novartis Institutes for Biomedical Research, 4560 Horton Street, Emeryville, CA 94608, USA.
Global Discovery Chemistry/Oncology & Exploratory Chemistry, Novartis Institutes for Biomedical Research, 4560 Horton Street, Emeryville, CA 94608, USA.
出版信息
Bioorg Med Chem Lett. 2014 Mar 15;24(6):1592-6. doi: 10.1016/j.bmcl.2014.01.058. Epub 2014 Jan 30.
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.
通过高通量筛选鉴定出2-氨基-7-取代苯并恶唑类似物为RSK2的抑制剂。采用分子建模和药物化学技术探索该系列的构效关系，重点是提高体外活性和靶点调节效力以及理化性质。
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