Córdoba Rubén, Tormo Nélida Salvador, Medarde Antonio Fernández, Plumet Joaquín
Departamento de Química Orgánica, Facultad de Químicas, Universidad Complutense, Madrid, Spain.
Bioorg Med Chem. 2007 Aug 1;15(15):5300-15. doi: 10.1016/j.bmc.2007.05.011. Epub 2007 May 6.
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.
合成了一系列具有潜在血管生成抑制作用的aeroplysinin-1 1类似物，并评估了它们的体外抗血管生成和细胞毒性活性。对于环氧酮6和恶唑酮36，相对于参考物，BAE细胞中的发芽抑制试验/细胞毒性关系分别提高了一个数量级和两个数量级。这些结果表明合成衍生物具有更特异的抗血管生成特性。
