Synthesis, binding and structure–affinity studies of new ligands for the microsomal anti-estrogen binding site (AEBS)

…, P De Medina, F Delarue, JJ Perie, A Klaebe…

Index: Poirot, Marc; De Medina, Philippe; Delarue, Frederic; Perie, Jean-Jacques; Klaebe, Alain; Faye, Jean-Charles Bioorganic and Medicinal Chemistry, 2000 , vol. 8, # 8 p. 2007 - 2016

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Citation Number: 27

Abstract

New compounds have been synthesized based on the structure of the anti-tumoral drug tamoxifen and its diphenylmethane derivative, N, N-diethyl-2-[(4-phenyl-methyl)-phenoxy]- ethanamine, HCl (DPPE). These new compounds have no affinity for the estrogen receptor (ER) and bind with various affinity to the anti-estrogen binding site (AEBS). Compounds 2, 10, 12, 13, 20a, 20b, 23a, 23b, 29 exhibited 1.1–69.5 higher affinity than DPPE, and ...