Molecular Basis for the Toxicity of Schweinfurthins to Breast Cancer cells
Abstract
The schweinfurthins are a small set of diprenylated stilbenes isolated from an African plant. Schweinfurthins A, and B display significant and unique activity in the NCI's 60 cell line panel, and the breast cancer lines MCF7 and HS 578T were among the most sensitive. We have developed multiple convergent routes to this family of compounds allowing an analog retaining anticancer activity to be synthesized as a single enantiomer. We have now synthesized a series of analogs including one bearing suitable functional groups for attachment to an affinity reagent or other reagent for determination of the mechanism of action. These studies have also led to synthetic analogs with more favorable stability, improving the ability to handle these agents. Quantitative structure activity studies have advanced our understanding of the essential pharmacophore and will pave the way for design of next generation analogs targeted at increasing the potency of the schweinfurthin family.
Document Details
- Document Type
- Technical Report
- Publication Date
- May 01, 2005
- Accession Number
- ADA437244
Entities
People
- David Wiemer
- Jeffrey Neighbors
Organizations
- University of Iowa