噻吩并[2,3-c]吡啶作为强效COT抑制剂的发现。
Discovery of thieno[2,3-c]pyridines as potent COT inhibitors.
作者信息
George Dawn, Friedman Michael, Allen Hamish, Argiriadi Maria, Barberis Claude, Bischoff Agnieszka, Clabbers Anca, Cusack Kevin, Dixon Richard, Fix-Stenzel Shannon, Gordon Thomas, Janssen Bernd, Jia Yong, Moskey Maria, Quinn Christopher, Salmeron Jose-Andres, Wishart Neil, Woller Kevin, Yu Zhengtian
机构信息
Abbott Bioresearch Center, 381 Plantation Street, Worcester, MA 01605, USA.
出版信息
Bioorg Med Chem Lett. 2008 Sep 15;18(18):4952-5. doi: 10.1016/j.bmcl.2008.08.037. Epub 2008 Aug 14.
Evaluation of hit chemotypes from high throughput screening identified a novel series of 2,4-disubstituted thieno[2,3-c]pyridines as COT kinase inhibitors. Structural modifications exploring SAR at the 2- and 4-positions resulting in inhibitors with improved enzyme potency and cellular activity are disclosed.
对高通量筛选得到的活性化学类型进行评估，确定了一系列新型的2,4-二取代噻吩并[2,3-c]吡啶作为COT激酶抑制剂。本文公开了在2位和4位探索构效关系的结构修饰，从而得到了酶活性和细胞活性均有所提高的抑制剂。
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