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Discovery of potent and selective Spleen Tyrosine Kinase inhibitors for the topical treatment of inflammatory skin disease
Bioorganic & Medicinal Chemistry Letters ( IF 2.7 ) Pub Date : 2018-09-18 , DOI: 10.1016/j.bmcl.2018.09.022
Michael D. Barker , John Liddle , Francis L. Atkinson , David Matthew Wilson , Marion C. Dickson , Cesar Ramirez-Molina , Huw Lewis , Rob P. Davis , Donald O. Somers , Margarete Neu , Emma Jones , Robert Watson

The discovery and lead optimisation of a novel series of SYK inhibitors is described. These were optimised for SYK potency and selectivity against Aurora B. Compounds were profiled in a human skin penetration study to identify a suitable candidate molecule for pre-clinical development. Compound 44 (GSK2646264) was selected for progression and is currently in Phase I clinical trials.



中文翻译:

发现有效和选择性的脾酪氨酸激酶抑制剂,用于局部治疗炎症性皮肤病

描述了一系列新型SYK抑制剂的发现和前导优化。这些化合物针对SYK效能和针对Aurora B的选择性进行了优化。在人类皮肤渗透研究中对化合物进行了分析,以鉴定出适合临床前开发的候选分子。选择化合物44(GSK2646264)进行治疗,目前处于I期临床试验中。

更新日期:2018-09-18
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