Antiangiogenic versus cytotoxic activity in analogues of aeroplysinin-1.
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.
Córdoba
Rubén
R
Departamento de Química Orgánica, Facultad de Químicas, Universidad Complutense, Madrid, Spain. rcordoba@pharmamar.com
Tormo
Nélida Salvador
NS
Medarde
Antonio Fernández
AF
Plumet
Joaquín
J
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
D000097:Acetonitriles; D000970:Antineoplastic Agents; D053138:Cyclohexenes; C042151:aeroplysinin I