双（吖啶基硫脲）铂（II）配合物：胶质母细胞瘤细胞中的合成、DNA亲和力及生物活性
Bis(acridinylthiourea)platinum(II) complexes: synthesis, DNA affinity, and biological activity in glioblastoma cells.
作者信息
Augustus Todd M, Anderson Joel, Hess Suzanne M, Bierbach Ulrich
机构信息
Department of Chemistry, Wake Forest University, Winston-Salem, NC 27109, USA.
出版信息
Bioorg Med Chem Lett. 2003 Mar 10;13(5):855-8. doi: 10.1016/s0960-894x(02)01078-8.
Abstract
The preparation of two novel bis(acridine)platinum(II) complexes is reported. The 4+ charged conjugates associate strongly with double-stranded native DNA (K(i)>10(6)), possibly through bisintercalation. A cell viability assay was used to demonstrate that both compounds are capable of mediating cytotoxicity at micromolar concentrations in SNB19 brain tumor cells.
摘要
报道了两种新型双（吖啶）铂（II）配合物的制备。带4 +电荷的共轭物与双链天然DNA强烈缔合（K(i)>10(6)），可能是通过双插入作用。使用细胞活力测定法证明这两种化合物在微摩尔浓度下都能够介导SNB19脑肿瘤细胞的细胞毒性。
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