Synthesis, biological evaluation, and docking studies of gigantol analogs as calmodulin inhibitors

…, T Serrano-Alba, M González-Andrade, R Mata

Index: Reyes-Ramirez, Adelfo; Leyte-Lugo, Martha; Figueroa, Mario; Serrano-Alba, Trinidad; Gonzalez-Andrade, Martin; Mata, Rachel European Journal of Medicinal Chemistry, 2011 , vol. 46, # 7 p. 2699 - 2708

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Citation Number: 8

Abstract

Abstract Several analogs of gigantol (1) were synthesized to evaluate their effect on the complexes Ca 2+–calmodulin (CaM) and Ca 2+–CaM–CaM sensitive phosphodiesterase 1 (PDE1). The compounds belong to four structural groups including, 1, 2-diphenylethanes (2– 11), diphenylmethanes (13–15), 1, 3-diphenylpropenones (16–18), and 1, 3- diphenylpropanes (20–22). In vitro enzymatic studies showed that all compounds except ...