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Synthesis of Pt(II) complexes of the type [Pt(1,10-phenanthroline)(SArFn)2] (SArFn = SC6H3-3,4-F2; SC6F4-4-H; SC6F5). Preliminary evaluation of their in vitro anticancer activity.
Journal of Inorganic Biochemistry ( IF 3.8 ) Pub Date : 2020-07-25 , DOI: 10.1016/j.jinorgbio.2020.111206
Geraldine Backman-Blanco 1 , Hugo Valdés 1 , María Teresa Ramírez-Apan 1 , Patricia Cano-Sanchez 1 , Simón Hernandez-Ortega 1 , Adrian L Orjuela 2 , Jorge Alí-Torres 2 , Areli Flores-Gaspar 3 , Reyna Reyes-Martínez 4 , David Morales-Morales 1
Affiliation  

A series of Pt(II) complexes of the type [Pt(1,10-phenanthroline)(SArFn)2] (SArFn = SC6H3-3,4-F2 (1); SC6F4-4-H (2); SC6F5 (3)) were synthesized from [Pt(1,10-phenanthroline)(Cl)2] and [Pb(SArFn)2] via metathesis reactions. The complexes were fully characterized including the unambiguous determination of their molecular structures by single-crystal X-ray diffraction techniques, showing the metal centers to be into a slightly distorted square-planar environments. The in vitro cytotoxic activity of the complexes was evaluated on six cancerous cell lines, i.e: glial cells of nervous central system (U-251), prostate (PC-3), leukemia (K-562), colon (HCT-15), breast (MCF-7) and lung (SKLU-1); we also included a healthy cell line of COS-7 (African green monkey kidney) for comparative purposes. We found that complex 2 was selective for PC-3. In addition, the IC50 values for the series of complexes were determined using the U-251, HCT-15 and SKLU-1 cancerous cell lines, as well as in the healthy cell line (COS-7), where complex 1 exhibited the best activity, with IC50 values going from 4.56 to 4.78 μM. These studies where further complemented with DNA docking theoretical calculations and DNA affinity experiments.



中文翻译:

合成[Pt(1,10-菲咯啉)(SArFn)2](SArFn = SC6H3-3,4-F2; SC6F4-4-H; SC6F5)类型的Pt(II)配合物。它们的体外抗癌活性的初步评估。

一系列的Pt(II)的类型[PT(1,10-菲咯啉)(SARF的络合物的Ñ2 ](SARF Ñ  = SC 6 H ^ 3 -3,4-F 2 (1) ; SC 6 ˚F 4 -通过[Pt(1,10-菲咯啉)(Cl)2 ]和[Pb(SArF n2 ]合成4-H (2) ; SC 6 F 5 (3)复分解反应。对该络合物进行了充分表征,包括通过单晶X射线衍射技术明确确定了它们的分子结构,表明金属中心处于略微扭曲的方平面环境中。在体外的复合物的细胞毒活性在六个癌细胞系,进行了评价,即:神经中央系统的神经胶质细胞(U-251),前列腺癌(PC-3),白血病(K-562),结肠(HCT-15) ,乳房(MCF-7)和肺(SKLU-1);为了进行比较,我们还包括一个健康的COS-7细胞系(非洲绿猴肾)。我们发现复合物2对PC-3具有选择性。另外,IC 50使用U-251,HCT-15和SKLU-1癌细胞系以及健康细胞系(COS-7)(其中配合物1表现出最佳活性)使用IC 50确定系列配合物的值值从4.56降至4.78μM。这些研究进一步辅以DNA对接理论计算和DNA亲和力实验。

更新日期:2020-08-12
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