title: Synthesis and antimitotic activity of novel 2-methoxyestradiol analogs. Part III.
abstract: The syntheses and antimitotic activity of several novel analogs of 2-methoxyestradiol are described. Structural modifications include ring-D homologation, aromatization of the six-membered ring-D to a chrysine type molecule, and introduction of unsaturation in five-membered ring-D along with substitution of alkyl and ethynyl groups for the 17beta-hydroxy function. Of nine analogs synthesized, five have demonstrated superior antiproliferative activities compared to 2-methoxyestradiol.
authors.affiliation: Department of Organic Chemistry, Southwest Foundation for Biomedical Research, P.O. Box 760549, 7620 NW Loop 410, San Antonio, TX 78245-0549, USA. pnrao@sfbr.org
authors.forename: Pemmaraju N
authors.initials: PN
authors.lastname: Rao
authors.forename: James W
authors.initials: JW
authors.lastname: Cessac
authors.forename: James W
authors.initials: JW
authors.lastname: Boyd
authors.forename: Arthur D
authors.initials: AD
authors.lastname: Hanson
authors.forename: Jamshed
authors.initials: J
authors.lastname: Shah
mesh_terms: D000077584:2-Methoxyestradiol; D050256:Antimitotic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D049109:Cell Proliferation / Q000187:drug effects; D002478:Cells, Cultured; D004730:Endothelium, Vascular / Q000166:cytology; D004958:Estradiol / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology; D006801:Humans; D020128:Inhibitory Concentration 50; D015394:Molecular Structure; D013329:Structure-Activity Relationship; D014471:Umbilical Veins
chemical_list: D050256:Antimitotic Agents; D004958:Estradiol; D000077584:2-Methoxyestradiol