Characterization of a novel bisacridone and comparison with PSC 833 as a potent and poorly reversible modulator of P-glycoprotein
JK Horton, KN Thimmaiah, GA Altenberg… - Molecular …, 1997 - Elsevier
Novel compounds, composed of two acridone moieties connected by a propyl or butyl
spacer, were synthesized and tested as potential modulators of P-glycoprotein (P-gp)-
mediated multidrug resistance. The propyl derivative 1, 3-bis (9-oxoacridin-10-yl)-propane
(PBA) was extremely potent and, at a concentration of 1 μ m, increased steady state
accumulation of vinblastine (VLB)≈ 9-fold in the multidrug-resistant cell line KB8–5. In
contrast to the readily reversible effects of VRP and cyclosporin A on VLB uptake and similar …
spacer, were synthesized and tested as potential modulators of P-glycoprotein (P-gp)-
mediated multidrug resistance. The propyl derivative 1, 3-bis (9-oxoacridin-10-yl)-propane
(PBA) was extremely potent and, at a concentration of 1 μ m, increased steady state
accumulation of vinblastine (VLB)≈ 9-fold in the multidrug-resistant cell line KB8–5. In
contrast to the readily reversible effects of VRP and cyclosporin A on VLB uptake and similar …