Synthesis, evaluation and absolute configuration assignment of novel dihydropyrimidin-2-ones as picomolar sodium iodide symporter inhibitors

P Lacotte, DA Buisson, Y Ambroise

Index: Lacotte, Pierre; Buisson, David-Alexandre; Ambroise, Yves European Journal of Medicinal Chemistry, 2013 , vol. 62, p. 722 - 727

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Citation Number: 11

Abstract

A small library of dihydropyrimidin-2-ones (DHPMs) was synthesized and evaluated for their potency to block iodide entrapment in rat thyroid cells. Synthesis was achieved using the multicomponent Biginelli reaction. Twelve compounds were tested for the inhibition of sodium iodide symporter (NIS) in a cell-based assay. One newly synthesized derivative exhibited a remarkably strong activity, with a half-maximum inhibitory concentration value ...