A new class of blockers of the voltage-gated potassium channel Kv1. 3 via modification of the 4-or 7-position of khellinone

…, JB Baell, N Toovey, D Homerick, H Wulff

Index: Harvey, Andrew J.; Baell, Jonathan B.; Toovey, Nathan; Homerick, Daniel; Wulff, Heike Journal of Medicinal Chemistry, 2006 , vol. 49, # 4 p. 1433 - 1441

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Citation Number: 29

Abstract

The voltage-gated potassium channel Kv1. 3 constitutes an attractive target for the selective suppression of effector memory T cells in autoimmune diseases. We have previously reported the natural product khellinone, 1a, as a versatile lead molecule and identified two new classes of Kv1. 3 blockers:(i) chalcone derivatives of khellinone, and (ii) khellinone dimers linked through the 6-position. Here we describe the multiple parallel synthesis of a ...