Benzosuberenes have highly potent anti-proliferative activity via inhibition of tubulin assembly at the colchicine binding site. Lead compounds include KGP18 and KGP156, which are potent small-molecule tubulin depolymerizing agents displaying sub-nanomolar (in the case of KGP18) antiproliferative activity in vitro against a number of human cancer cell lines. These compounds have also been shown to disrupt capillary-like networks of endothelial cells in vitro and induce reductions in tumor blood flow in human tumor xenografts in mice. Two publications detailing the synthesis and in vitro activity of the initial lead compounds in this series of benzosuberenes have appeared in print ( Bioorg. Med. Chem. 16:8161-8171 (2008); and Med. Chem. Commun. 3:720-24 (2012).About OXiGENE
OXiGENE Announces Issuance Of Patent For Benzosuberenes, A Novel Anticancer Class Of Agents
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