Novel insight in structure-activity relationship and bioanalysis of P-glycoprotein targeting highly potent tetrakishydroxymethyl substituted 3,9-diazatetraasteranes

Journal of Medicinal Chemistry
Claudius CoburgerAndreas Hilgeroth

Abstract

Novel 3,9-diazatetraasteranes have been synthesized with varied aromatic substitution patterns and evaluated as P-glycoprotein (P-gp) inhibitors. Structure-activity relationships (SAR) are discussed in relation to determined physicochemical properties. The potential to induce P-gp expression has been evaluated in cancer cell lines. The bioanalytical results indicate favorable noninducing properties compared to P-gp inducing drug standard.

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Citations

Nov 3, 2011·Biochemical Pharmacology·Andreia PalmeiraEmília Sousa
Nov 9, 2010·The Journal of Pharmacy and Pharmacology·Claudius CoburgerAndreas Hilgeroth
Feb 9, 2012·Natural Product Communications·Ai-Ying GuanHong Zhang
Mar 23, 2018·Beilstein Journal of Organic Chemistry·Alexey M StarosotnikovIgor L Dalinger

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