title: 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.
authors.affiliation: Department of Chemistry, University of Iowa, Iowa City, IA 52242-1294, United States.
authors.forename: John G
authors.initials: JG
authors.lastname: Kodet
authors.affiliation: Molecular Targets Laboratory, Center for Cancer Research, NCI-Frederick, Frederick, MD 21702, United States.
authors.forename: John A
authors.initials: JA
authors.lastname: Beutler
authors.affiliation: Department of Chemistry, University of Iowa, Iowa City, IA 52242-1294, United States. Electronic address: david-wiemer@uiowa.edu.
authors.forename: David F
authors.initials: DF
authors.lastname: Wiemer
mesh_terms: D000970:Antineoplastic Agents / Q000494:pharmacology; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D007211:Indoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D013267:Stilbenes / Q000737:chemistry*; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D007211:Indoles; D013267:Stilbenes; C030374:indole
keywords: Indole; SAR; Schweinfurthin; Stilbene analogues