pgp - publications

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Activity-lipophilicity relationship studies on P-gp ligands designed as simplified tariquidar bulky fragments.

Bioorg Med Chem Lett. 2013 May 16;

Authors: Contino M, Zinzi L, Cantore M, Perrone MG, Leopoldo M, Berardi F, Perrone R, Colabufo NA


A series of alkyloxyquinoline derivatives has been developed to evaluate the relationship between P-gp potency and lipophilicity. The results show a satisfactory lipophilicity-activity correlation although a series of derivatives showing higher P-gp potency is needed in order to confirm this hypothesis.

PMID: 23726026 [PubMed - as supplied by publisher]