Synthesis and evaluation of a novel nonsteroidal-specific endothelial cell proliferation inhibitor.
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.
Schmidt
Jonathan M
JM
SignalGene Inc., Unit 2, 335 Laird Road, Guelph, Ontario N1G 4P7, Canada.
Tremblay
Gilles B
GB
Pagé
Martine
M
Mercure
Julie
J
Feher
Miklos
M
Dunn-Dufault
Robert
R
Peter
Markus G
MG
Redden
Peter R
PR
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
D020533:Angiogenesis Inhibitors; D047628:Estrogen Receptor alpha; D047629:Estrogen Receptor beta; D011714:Pyrans; D011960:Receptors, Estrogen; D004958:Estradiol; D000077584:2-Methoxyestradiol