4-Phenoxybutoxy-substituted heterocycles–A structure–activity relationship study of blockers of the lymphocyte potassium channel Kv1. 3

SB Bodendiek, C Mahieux, W Hänsel, H Wulff

文献索引：Bodendiek, Silke B.; Mahieux, Cedrick; Haensel, Wolfram; Wulff, Heike European Journal of Medicinal Chemistry, 2009 , vol. 44, # 5 p. 1838 - 1852

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被引用次数: 31

摘要

The voltage-gated potassium channel Kv1. 3 constitutes an attractive pharmacological target for the treatment of effector memory T cell-mediated autoimmune diseases such as multiple sclerosis and psoriasis. Using 5-methoxypsoralen (5-MOP, 1), a compound isolated from Ruta graveolens, as a template we previously synthesized 5-(4-phenoxybutoxy) psoralen (PAP-1, 2) which inhibits Kv1. 3 with an IC50 of 2nM. Since PAP-1 is more than 1000-fold ...