Synthesis and Biological Evaluation of (−)-Laulimalide Analogues
2003; American Chemical Society; Volume: 5; Issue: 19 Linguagem: Inglês
10.1021/ol035339f
ISSN1523-7060
AutoresPaul A. Wender, Sayee G. Hegde, Robert D. Hubbard, Lei Zhang, Susan L. Mooberry,
Tópico(s)Traditional and Medicinal Uses of Annonaceae
ResumoThe syntheses of five laulimalide analogues are described, incorporating modifications at the C16−C17-epoxide, the C20-alcohol, as well as the C1−C3-enoate of the parent natural product. The resultant analogues are active in drug-sensitive HeLa and MDA-MB-435 cell lines. Significantly, like laulimalide, these analogues are poor substrates for the drug transport protein P-glycoprotein (Pgp) and are thus effective against Taxol-resistant cell lines.
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