Dual inhibitors of P-glycoprotein and tumor cell growth:(re) discovering thioxanthones

…, A Paiva, MX Fernandes, M Pinto, E Sousa

Index: Palmeira, Andreia; Vasconcelos, M. Helena; Paiva, Ana; Fernandes, Miguel X.; Pinto, Madalena; Sousa, Emilia Biochemical Pharmacology, 2012 , vol. 83, # 1 p. 57 - 68

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Citation Number: 58

Abstract

For many pathologies, there is a crescent effort to design multiple ligands that interact with a wide variety of targets. 1-Aminated thioxanthone derivatives were synthesized and assayed for their in vitro dual activity as antitumor agents and P-glycoprotein (P-gp) inhibitors. The approach was based on molecular hybridization of a thioxanthone scaffold, present in known antitumor drugs, and an amine, described as an important pharmacophoric feature ...