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Synthesis and structure activity relationships of schweinfurthin indoles.

ABSTRACT: As part of a program to explore the biological activity of analogues of the natural schweinfurthins, a set of compounds has been prepared where an indole system can be viewed as a substitution for the resorcinol substructure of the schweinfurthin's D-ring. Twelve of these schweinfurthin indoles have been prepared and evaluated in the 60 cell line screen of the National Cancer Institute. While a range of activity has been observed, it is now clear that schweinfurthin indoles can demonstrate the intriguing pattern of activity associated with the natural stilbenes. In the best cases, these indole analogues display both potency and differential activity across the various cell lines comparable to the best resorcinol analogues.

SUBMITTER: Kodet JG

PROVIDER: S-EPMC4030441 | biostudies-literature | 2014 Apr

REPOSITORIES: biostudies-literature

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Synthesis and structure activity relationships of schweinfurthin indoles.

Kodet John G JG Beutler John A JA Wiemer David F DF

Bioorganic & medicinal chemistry 20140306 8

As part of a program to explore the biological activity of analogues of the natural schweinfurthins, a set of compounds has been prepared where an indole system can be viewed as a substitution for the resorcinol substructure of the schweinfurthin's D-ring. Twelve of these schweinfurthin indoles have been prepared and evaluated in the 60 cell line screen of the National Cancer Institute. While a range of activity has been observed, it is now clear that schweinfurthin indoles can demonstrate the i ...[more]

PMID: 24656801

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