Literature

Abstract

To search multi drug resistance modulators, acridones carrying hydroxyl amine substituent at N-10 and COOH/Cl at C-4 were investigated for their interactions with the three components of efflux pump viz. P-gp, ATP, and Mg(2+). Experimental and theoretical results indicated that the compounds with COOH group at C-4 interact with P-gp and Mg(2+) while other set of compounds with Cl at C-4 interact with ATP and Mg(2+). Spot assay and R6G influx/efflux assay of compound 3 using Candida albicans showed decrease in the fungal growth and efflux of R6G, respectively, in presence of compound 3 suggesting the suitability of this compound for MDR modulation.

DOI： 10.1016/j.bmc.2010.05.003

Targeting efflux pumps—In vitro investigations with acridone derivatives and identification of a lead molecule for MDR modulation

Bioorganic & Medicinal Chemistry 2010.0

Search for MDR modulators: Design, syntheses and evaluations of N-substituted acridones for interactions with p-glycoprotein and Mg2+

Bioorganic & Medicinal Chemistry 2009.0

Design, synthesis and evaluations of acridone derivatives using Candida albicans—Search for MDR modulators led to the identification of an anti-candidiasis agent

Bioorganic & Medicinal Chemistry 2009.0

Acridones circumvent P-glycoprotein-associated multidrug resistance (MDR) in cancer cells

Bioorganic & Medicinal Chemistry 2008.0

The 5-aromatic hydantoin-3-acetate derivatives as inhibitors of the tumour multidrug resistance efflux pump P-glycoprotein (ABCB1): Synthesis, crystallographic and biological studies

Bioorganic & Medicinal Chemistry 2016.0

From mixed sigma-2 receptor/P-glycoprotein targeting agents to selective P-glycoprotein modulators: Small structural changes address the mechanism of interaction at the efflux pump