Department of Chemistry, University of Warwick, Coventry, UK.
Dalton Trans. 2010 Dec 21;39(47):11353-64. doi: 10.1039/c0dt00838a. Epub 2010 Oct 29.
A range of androgen conjugates with non-conventional platinum(II) complexes have been synthesised with the aim of targeting tumour cells since many display elevated levels of the androgen receptor. The androgenic platinum conjugates are delivered into selected cells with improved efficiency (when compared to their non-steroidal analogues). The act of conjugating an androgen to a platinum(II) complex resulted in synergistic effects between the metallic centre and the steroidal ligand, creating highly potent platinum(II) complexes from the inactive components.
已经合成了一系列具有非传统铂(II)配合物的雄激素缀合物,旨在针对肿瘤细胞,因为许多肿瘤细胞显示出高水平的雄激素受体。与非甾体类似物相比,雄激素结合铂(II)配合物以更高的效率递送到选定的细胞中。将雄激素与铂(II)配合物缀合导致金属中心和甾体配体之间产生协同作用,从而使原本无活性的成分形成高效的铂(II)配合物。