SAR study on Arylmethyloxyphenyl scaffold: looking for a P-gp nanomolar affinity

…, R Perrone, A Lapucci, M Macchia, S Rapposelli

Index: Nesi, Giulia; Colabufo, Nicola Antonio; Contino, Marialessandra; Perrone, Maria Grazia; Digiacomo, Maria; Perrone, Roberto; Lapucci, Annalina; Macchia, Marco; Rapposelli, Simona European Journal of Medicinal Chemistry, 2014 , vol. 76, p. 558 - 566

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Citation Number: 3

Abstract

Abstract Starting from the previously developed P-gp ligands 1a and 1b (EC 50= 0.25 μM and 0.65 μM, respectively), new arylmethyloxyphenyl derivatives have been synthesized as P-gp modulators in order to investigate:(i) the effect of small electron-donor groups (OMe)(5– 11),(ii) the effect of the replacement of methoxy groups with an electron-withdrawal substituent (Cl) on C-ring (13)(iii) the effect induced by the replacement of C-ring with ...