Volume 27, Issue 23
Isocyclic Compounds
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ChemInform Abstract: Homologues of Idoxifene (Ia): Variation of Estrogen Receptor Binding and Calmodulin Antagonism with Chain Length.

I. R. HARDCASTLE

I. R. HARDCASTLE

CRC Cent. Cancer Ther., Cancer Res. Campaign Lab., Inst. Cancer Res., Sutton, Surrey SM2 5NG, UK

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M. G. ROWLANDS

M. G. ROWLANDS

CRC Cent. Cancer Ther., Cancer Res. Campaign Lab., Inst. Cancer Res., Sutton, Surrey SM2 5NG, UK

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R. M. GRIMSHAW

R. M. GRIMSHAW

CRC Cent. Cancer Ther., Cancer Res. Campaign Lab., Inst. Cancer Res., Sutton, Surrey SM2 5NG, UK

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J. HOUGHTON

J. HOUGHTON

CRC Cent. Cancer Ther., Cancer Res. Campaign Lab., Inst. Cancer Res., Sutton, Surrey SM2 5NG, UK

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M. JARMAN

M. JARMAN

CRC Cent. Cancer Ther., Cancer Res. Campaign Lab., Inst. Cancer Res., Sutton, Surrey SM2 5NG, UK

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A. SHARFF

A. SHARFF

CRC Cent. Cancer Ther., Cancer Res. Campaign Lab., Inst. Cancer Res., Sutton, Surrey SM2 5NG, UK

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S. NEIDLE

S. NEIDLE

CRC Cent. Cancer Ther., Cancer Res. Campaign Lab., Inst. Cancer Res., Sutton, Surrey SM2 5NG, UK

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First published: June 4, 1996

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).

chemical structure image

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