Abstract:
:Dimethylallyl (DMA) derivatives of a naturally occurring xanthone (decussatin 1) were prepared. Their activity as potential P-glycoprotein inhibitors was monitored by affinity of direct binding and compared to that of corresponding DMA-flavones. Both classes of compounds exhibited the same structure-activity relationships. Decreasing polarity enhanced the binding affinity for the P-glycoprotein C-terminal cytosolic domain since DMA derivatives were more active, but unsubstituted hydroxyl group close to the carbonyl was required for efficient activity.
journal_name
Bioorg Med Chem Lettjournal_title
Bioorganic & medicinal chemistry lettersauthors
Tchamo DN,Dijoux-Franca MG,Mariotte AM,Tsamo E,Daskiewicz JB,Bayet C,Barron D,Conseil G,Di Pietro Adoi
10.1016/s0960-894x(00)00234-1subject
Has Abstractpub_date
2000-06-19 00:00:00pages
1343-5issue
12eissn
0960-894Xissn
1464-3405pii
S0960-894X(00)00234-1journal_volume
10pub_type
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