… receptor ligand 1-cyclohexyl-4-[3-(5-methoxy-1, 2, 3, 4-tetrahydronaphthalen-1-yl) propyl] piperazine (PB28) with added polar functionality and reduced lipophilicity for …

…, M Niso, E Lacivita, PD Mosier, A Toscano…

Index: Abate, Carmen; Niso, Mauro; Lacivita, Enza; Mosier, Philip D.; Toscano, Annamaria; Perrone, Roberto Journal of Medicinal Chemistry, 2011 , vol. 54, # 4 p. 1022 - 1032

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Citation Number: 19

Abstract

1-Cyclohexyl-4-[3-(5-methoxy-1, 2, 3, 4-tetrahydronaphthalen-1-yl) propyl] piperazine 1 (PB28) represents an excellent lead candidate for therapeutic and/or diagnostic applications in oncology. However, because its utility is limited by its relatively high degree of lipophilicity, novel analogues of 1 with reduced lipophilic character were designed by substituting methylene groups with more polar functional groups in the propylene linker and at the ...