2. Academic Validation
  3. Synthesis and evaluation of hapalosin and analogs as MDR-reversing agents

Synthesis and evaluation of hapalosin and analogs as MDR-reversing agents

  • Bioorg Med Chem Lett. 1999 Jun 7;9(11):1541-6. doi: 10.1016/s0960-894x(99)00243-7.
C E O'Connell 1,  K A Salvato,  Z Meng,  B A Littlefield,  C E Schwartz
Affiliations

Affiliation

  • 1 Eisai Research Institute, Andover, MA 01810, USA.
PMID: 10386932 DOI: 10.1016/s0960-894x(99)00243-7
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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