Screening of Natural Compounds as P-Glycoprotein Inhibitors against Multidrug Resistance

Multidrug Resistance Protein (P-Glycoprotein; MDR1)

Design, synthesis, and biological evaluation of 6-methoxy-2-arylquinolines as potential P-glycoprotein inhibitors

Objective(s): In the present study,a new series of 6-methoxy-2-arylquinoline analogues was designed and synthesized as P-glycoprotein (P-gp) inhibitors using quinine and flavones as the lead compounds. Materials and Methods: The cytotoxic activity of the synthesized compounds was evaluated against two human cancer cell lines including EPG85-257RDB, multidrug-resistant gastric carcinoma cells (P...

Molecular Mimics of Classic P-Glycoprotein Inhibitors as Multidrug Resistance Suppressors and Their Synergistic Effect on Paclitaxel

P-glycoprotein (Pgp) is a membrane bound efflux pump spread in a variety of tumor cells and considered as a main component of multidrug resistance (MDR) to chemotherapies. In this work, three groups of compounds (imidazolone, oxazolone and vinyl dipeptide derivatives) were synthesized aiming to develop a molecular framework that effectively suppresses MDR. When tested for their influence on Pgp...

Inhibition of P-glycoprotein mediated multidrug resistance by stemofoline derivatives.

Resistance to chemotherapy in cancer patients has been correlated to the overexpression of the ATP-binding cassette (ABC) drug transporters including P-glycoprotein (P-gp) that actively efflux chemotherapeutic drugs from cancer cells. We examined the multidrug resistance reversing property of stemofoline derivatives in drug-resistance human cervical carcinoma (KB-V1) and human leukemic (K562/Ad...

Role of ABCB5 P-glycoprotein in Breast Cancer Multidrug Resistance

Rigol N, Frank NY, Margaryan A, Schatton T, Frank MH. Differential expression of ABCB5 multidrug resistance P-glycoprotein in human breast cancer cell lines. Proceedings of the Department of Defense Breast Cancer Research Program Meeting (Era of Hope), June 8-11, 2005, Philadelphia, PA. 2005:467 Abstract P667.