Synthesis and evaluation of hapalosin and analogs as MDR-reversing agents. |
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Authors: | C E O'Connell K A Salvato Z Meng B A Littlefield C E Schwartz |
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Affiliation: | Eisai Research Institute, Andover, MA 01810, USA. |
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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. |
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