title: Synthesis and evaluation of a novel nonsteroidal-specific endothelial cell proliferation inhibitor.
abstract: The identification of agents with specific antiproliferative or cytostatic activity against endothelial cells has significant value for the treatment of pathologies associated with angiogenesis, including solid tumors. Here, we describe a novel substituted dibenzo[b,d]pyran-6-one scaffold, exemplified by structures 9a and 10, and report preliminary in vitro activity data indicating that this scaffold is a promising lead for the development of specific inhibitors of endothelial cell proliferation.
authors.affiliation: SignalGene Inc., Unit 2, 335 Laird Road, Guelph, Ontario N1G 4P7, Canada.
authors.forename: Jonathan M
authors.initials: JM
authors.lastname: Schmidt
authors.forename: Gilles B
authors.initials: GB
authors.lastname: Tremblay
authors.forename: Martine
authors.initials: M
authors.lastname: Pagé
authors.forename: Julie
authors.initials: J
authors.lastname: Mercure
authors.forename: Miklos
authors.initials: M
authors.lastname: Feher
authors.forename: Robert
authors.initials: R
authors.lastname: Dunn-Dufault
authors.forename: Markus G
authors.initials: MG
authors.lastname: Peter
authors.forename: Peter R
authors.initials: PR
authors.lastname: Redden
mesh_terms: D000077584:2-Methoxyestradiol; D020533:Angiogenesis Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D001667:Binding, Competitive; D002455:Cell Division / Q000187:drug effects; D003198:Computer Simulation; D004730:Endothelium, Vascular / Q000166:cytology / Q000187:drug effects*; D004958:Estradiol / Q000031:analogs & derivatives / Q000737:chemistry / Q000494:pharmacology; D047628:Estrogen Receptor alpha; D047629:Estrogen Receptor beta; D006801:Humans; D008958:Models, Molecular; D011714:Pyrans / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D011960:Receptors, Estrogen / Q000378:metabolism; D013329:Structure-Activity Relationship; D014407:Tumor Cells, Cultured; D014471:Umbilical Veins / Q000166:cytology
chemical_list: D020533:Angiogenesis Inhibitors; D047628:Estrogen Receptor alpha; D047629:Estrogen Receptor beta; D011714:Pyrans; D011960:Receptors, Estrogen; D004958:Estradiol; D000077584:2-Methoxyestradiol