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Discovery of 5,6,7,8-tetrahydropyrido[3,4-d]pyrimidine inhibitors of Erk2
Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2014-04-29 , DOI: 10.1016/j.bmcl.2014.04.068 James F. Blake , John J. Gaudino , Jason De Meese , Peter Mohr , Mark Chicarelli , Hongqi Tian , Rustam Garrey , Allen Thomas , Christopher S. Siedem , Michael B. Welch , Gabrielle Kolakowski , Robert Kaus , Michael Burkard , Matthew Martinson , Huifen Chen , Brian Dean , Danette A. Dudley , Stephen E. Gould , Patricia Pacheco , Sheerin Shahidi-Latham , Weiru Wang , Kristina West , Jianping Yin , John Moffat , Jacob B. Schwarz
中文翻译：
发现Erk2的5,6,7,8-四氢吡啶并[3,4- d ]嘧啶抑制剂
更新日期：2014-04-29
Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2014-04-29 , DOI: 10.1016/j.bmcl.2014.04.068 James F. Blake , John J. Gaudino , Jason De Meese , Peter Mohr , Mark Chicarelli , Hongqi Tian , Rustam Garrey , Allen Thomas , Christopher S. Siedem , Michael B. Welch , Gabrielle Kolakowski , Robert Kaus , Michael Burkard , Matthew Martinson , Huifen Chen , Brian Dean , Danette A. Dudley , Stephen E. Gould , Patricia Pacheco , Sheerin Shahidi-Latham , Weiru Wang , Kristina West , Jianping Yin , John Moffat , Jacob B. Schwarz
The discovery and optimization of a series of tetrahydropyridopyrimidine based extracellular signal-regulated kinase (Erks) inhibitors discovered via HTS and structure based drug design is reported. The compounds demonstrate potent and selective inhibition of Erk2 and knockdown of phospho-RSK levels in HepG2 cells and tumor xenografts.
中文翻译：
发现Erk2的5,6,7,8-四氢吡啶并[3,4- d ]嘧啶抑制剂
报道了通过HTS和基于结构的药物设计发现的一系列基于四氢吡啶并嘧啶的细胞外信号调节激酶（Erks）抑制剂的发现和优化。该化合物在HepG2细胞和肿瘤异种移植物中显示出对Erk2的有效和选择性抑制，并降低了磷酸-RSK水平。
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