合成、抗增殖活性和作为潜在抗乳腺癌药物的镓（III）-缩氨硫脲配合物的机制。
Synthesis, antiproliferative activity and mechanism of gallium(III)-thiosemicarbazone complexes as potential anti-breast cancer agents.
机构信息
School of Chemistry and Chemical Engineering, Southeast University, Nanjing, 211189, China.
Stanford Cancer Institute, Member of Academic Council, Stanford University, USA.
出版信息
Eur J Med Chem. 2018 Jun 25;154:91-100. doi: 10.1016/j.ejmech.2018.05.016. Epub 2018 May 14.
Five thiosemicarbazone ligands were synthesized and characterized by condensation with different aldehydes or ketones by 4-phenylthiosemicarbazone. The representative dichlorido[2-(Di-2-pyridinylmethylene)-Nphenylhydrazinecarbothioamide-N,N,S]-gallium(III) (Ga4) was characterized by X-ray single crystal diffraction, which was 1:1 ligand/Ga(III) complexes. The structure-activity relationship of these ligands and Ga (III) complexes have been investigated, and the results demonstrate that the formation of Ga (III) complexes have significant antiproliferative activity over the corresponding ligands. The anticancer mechanism of gallium (III) complexes has been studied in detail, which is typical agents that effect on the mitochondrial apoptotic pathway. The ability of gallium (III) complexes to inhibit the cell cycle does not enhanced with the increasing concentrations, whereas the ability to promote apoptosis is concentration-dependent.
合成了 5 种缩氨基硫脲配体，通过 4-苯硫代缩氨基脲与不同的醛或酮缩合得到。以二吡啶亚甲基-N-苯基腙硫代甲酰胺（H2L）为配体，合成了一个具有代表性的二氯[2-（二吡啶基亚甲基）-N-苯基腙硫代甲酰胺-N，N，S]-镓（III）（Ga4）配合物。通过 X 射线单晶衍射对其结构进行了表征，该配合物为 1:1 配体/镓（III）配合物。研究了这些配体和 Ga（III）配合物的构效关系，结果表明，Ga（III）配合物的形成对相应配体具有显著的抗增殖活性。详细研究了镓（III）配合物的抗癌机制，这是一种典型的作用于线粒体凋亡途径的药物。镓（III）配合物抑制细胞周期的能力并不随浓度的增加而增强，而促进凋亡的能力则是浓度依赖性的。
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