ChemInform Abstract: Homologues of Idoxifene (Ia): Variation of Estrogen Receptor Binding and Calmodulin Antagonism with Chain Length.
Abstract
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ChemInform Abstract
A series (14 examples) of homologues of idoxifene (Ia) and 4- iodotamoxifen (If) with side chains up to length (-CH2-)10 are prepared as illustrated for derivative (Id) and tested for antagonism of the calmodulin-dependent activity of cAMP phosphodiesterase and for binding affinity to rat uterine estrogen receptor. Compared to (Ia) ( IC50 = 1.5 μM), the homologues exhibit a progressive increase in calmodulin antagonism with a maximum inhibition for (Ic)-(Ie) (IC50 = 0.2 μM). The estrogen receptor binding affinity is the highest for ( Ib).