Synthesis and evaluation of hapalosin and analogs as MDR-reversing agents.
Article Details
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O'Connell CE, Salvato KA, Meng Z, Littlefield BA, Schwartz CE
Synthesis and evaluation of hapalosin and analogs as MDR-reversing agents.
Bioorg Med Chem Lett. 1999 Jun 7;9(11):1541-6.
- PubMed ID
- 10386932 [ View in PubMed]
- Abstract
The marine natural product hapalosin and 22 analogs, which incorporated systematic substituent deletions or variations, were prepared. These compounds were evaluated in a cell-based assay for both MDR-reversing activity and general cytotoxicity. Some substituent modifications resulted in lower cytotoxicities, but most structural changes were either detrimental to or did not seriously alter the MDR-reversing activity.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Verapamil P-glycoprotein 1 IC 50 (nM) 3100 N/A N/A Details Verapamil P-glycoprotein 1 IC 50 (nM) 53000 N/A N/A Details