title: Antiangiogenic versus cytotoxic activity in analogues of aeroplysinin-1.
abstract: A series of analogues of the potentially angiogenic inhibitor aeroplysinin-1 1 were synthesized and their in vitro antiangiogenic and cytotoxic activities evaluated. In the case of epoxy ketone 6 and azlactone 36 the relationship sprouting inhibition assay/cytotoxicity in BAE cells was enhanced by one order and two orders of magnitude, respectively, with respect to the reference. These results imply more specific antiangiogenic properties for the synthesized derivatives.
authors.affiliation: Departamento de Química Orgánica, Facultad de Químicas, Universidad Complutense, Madrid, Spain. rcordoba@pharmamar.com
authors.forename: Rubén
authors.initials: R
authors.lastname: Córdoba
authors.forename: Nélida Salvador
authors.initials: NS
authors.lastname: Tormo
authors.forename: Antonio Fernández
authors.initials: AF
authors.lastname: Medarde
authors.forename: Joaquín
authors.initials: J
authors.lastname: Plumet
mesh_terms: D000097:Acetonitriles / Q000737:chemistry* / Q000494:pharmacology*; D000818:Animals; D000970:Antineoplastic Agents / Q000737:chemistry* / Q000494:pharmacology*; D002417:Cattle; D002478:Cells, Cultured; D053138:Cyclohexenes / Q000737:chemistry* / Q000494:pharmacology*; D042783:Endothelial Cells / Q000166:cytology / Q000187:drug effects* / Q000378:metabolism; D020128:Inhibitory Concentration 50; D008968:Molecular Conformation; D018919:Neovascularization, Physiologic / Q000187:drug effects*; D013329:Structure-Activity Relationship
chemical_list: D000097:Acetonitriles; D000970:Antineoplastic Agents; D053138:Cyclohexenes; C042151:aeroplysinin I