Rationally designed analogs of tamoxifen with improved calmodulin antagonism

IR Hardcastle, MG Rowlands, J Houghton…

Index: Hardcastle; Rowlands; Houghton; Parr; Potter; Jarman; Edwards; Laughton; Trent; Neidle Journal of Medicinal Chemistry, 1995 , vol. 38, # 2 p. 241 - 248

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Citation Number: 49

Abstract

Computerized molecular modeling studies on the interactions of the antiestrogen tamoxifen (1) and its analogues bound to the calcium-binding protein calmodulin have guided the rational design of more potent antagonists. Compounds with either three or four methylene units in the basic side chain or slim lipophilic 4-substituents were expected to be more potent. All compounds were tested for antagonism of the calmodulin-dependent activity of ...