Kheradi Alexander R, Saluta Gilda, Kucera Gregory L, Day Cynthia S, Bierbach Ulrich
Department of Chemistry, Wake Forest University, Winston-Salem, NC 27109, USA.
Bioorg Med Chem Lett. 2009 Jul 1;19(13):3423-5. doi: 10.1016/j.bmcl.2009.05.046. Epub 2009 May 18.
The use of 2,2'-bipyridines (4,4'-R(2)-2,2'-bpy; R=H, Me, OMe, CF(3)) as non-leaving groups (L-L) in platinum-acridinylthiourea conjugates, PtCl(L-L)(ACRAMTU)(2), has been investigated. All bpy-substituted complexes (2-5) show micromolar activity in HL-60 (leukemia) and H460 (lung) cancer cell lines but proved to be significantly less potent than the prototypical compound (1) containing aliphatic ethane-1,2-diamine. NMR and mass spectrometry data indicate that bpy accelerates the reaction of platinum with DNA nitrogen, but the resulting adducts are more labile than those formed by the prototype.
研究了在铂-吖啶基硫脲共轭物PtCl(L-L)(ACRAMTU)₂中使用2,2'-联吡啶（4,4'-R(2)-2,2'-bpy；R = H、Me、OMe、CF₃）作为非离去基团（L-L）的情况。所有联吡啶取代的配合物（2-5）在HL-60（白血病）和H460（肺癌）癌细胞系中均表现出微摩尔活性，但事实证明其效力明显低于含有脂肪族乙烷-1,2-二胺的原型化合物（1）。核磁共振和质谱数据表明，联吡啶加速了铂与DNA氮的反应，但生成的加合物比原型形成的加合物更不稳定。
