کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
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1360096 | 981424 | 2010 | 12 صفحه PDF | دانلود رایگان |
![عکس صفحه اول مقاله: Targeting efflux pumps—In vitro investigations with acridone derivatives and identification of a lead molecule for MDR modulation Targeting efflux pumps—In vitro investigations with acridone derivatives and identification of a lead molecule for MDR modulation](/preview/png/1360096.png)
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 Mg2+. Experimental and theoretical results indicated that the compounds with COOH group at C-4 interact with P-gp and Mg2+ while other set of compounds with Cl at C-4 interact with ATP and Mg2+. 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.
Acridone based molecules are identified for blocking the drug efflux pumps either through interactions with P-gp/cdr1p/cdr2p or interacting with ATP/Mg2+.Figure optionsDownload as PowerPoint slide
Journal: Bioorganic & Medicinal Chemistry - Volume 18, Issue 12, 15 June 2010, Pages 4212–4223