cis-[Pt(dichloroacetate)₂(NH₃)₂] | 1421629-47-1

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: cis-[Pt(dichloroacetate)₂(NH₃)₂]
• CAS: 1421629-47-1
• 化学式: C₄H₈Cl₄N₂O₄Pt
• 分子量: 485.011
• InChiKey: DTCRWEGBLUBMRI-UHFFFAOYSA-L

计算性质

• 辛醇/水分配系数(LogP)：
  None
• 重原子数：
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• 可旋转键数：
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• 环数：
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• sp3杂化的碳原子比例：
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• 拓扑面积：
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• 氢给体数：
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• 氢受体数：
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反应信息

• 作为产物：
  描述：

  sodium dichloroacetate 、 cisplatin 在 硝酸 、 silver nitrate 作用下， 以 水 为溶剂， 反应 48.0h， 以87%的产率得到cis-[Pt(dichloroacetate)₂(NH₃)₂]
  参考文献：
  名称：

  A hybrid platinum drug dichloroacetate-platinum(II) overcomes cisplatin drug resistance through dual organelle targeting

  摘要：

  A hybrid drug dichloroacetate-platinum(II) [DCA-Pt(II)] was found to overcome cisplatin drug resistance of ovarian cancer through a dual targeting mode, which is different from the mode of action of the present platinum (Pt) drugs used in clinics. DCA-Pt(II) exhibited remarkable cytotoxicity against both cisplatin-sensitive (A2780) and cisplatin-resistant (A2780DDP) ovarian cancer cells. The Pt and Pt-DNA adduct content test showed that there was less Pt cellular uptake and fewer Pt-DNA adducts were present after DCA-Pt(II) treatment compared with treatment with cisplatin, carboplatin, and some other drugs. In the study, the effects of DCA-Pt(II) on the cell cycle and apoptosis were also investigated, which showed that DCA-Pt(II) induced G2/M phase arrest and mitochondria-mediated apoptosis in both sensitive and resistant cells lines. Interestingly, DCA-Pt(II) had much greater effects on mitochondria in A2780DDP cell lines than in A2780 cell lines.

  DOI：

  10.1097/cad.0000000000000234

文献信息

• Synthesis and characterization of Pt complexes containing dichloroacetate (DCA), designed for dual anticancer action
  作者：Valeria Ferretti、Paola Bergamini、Lorenza Marvelli、Yekatsiaryna Hushcha、Chiara Gemmo、Roberto Gambari、Ilaria Lampronti

  DOI：10.1016/j.ica.2017.04.048

  日期：2018.1

  dichloroacetate (DCA), bearing DMSO ( cis -[Pt(DCA) 2 (Me 2 SO -S ) 2 ], 2 ) or phosphines ( cis -[Pt(DCA) 2 (PPh 3 )(Me 2 SO -S )], 3 , cis -[Pt(DCA) 2 (P) 2 ], P = PPh 3 3a , P = PTA 4a and [Pt(DCA)(P) 3 ]DCA, P = PPh 3 3b , P = PTA, 4b ) as neutral ligands was prepared by a simple fast route from the inorganic synthon [PtCO 3 (Me 2 SO -S ) 2 ], 1 . The X-ray crystal structures of 2 , 3 , 3a and 4a were

  摘要一组新的带有二氯乙酸酯（DCA）的Pt（II）配合物，带有DMSO（顺式-[Pt（DCA）2（Me 2 SO -S）2]，2）或膦（顺式-[Pt（DCA）2） （PPh 3）（Me 2 SO -S）]，3，顺式-[Pt（DCA）2（P）2]，P = PPh 3 3a，P = PTA 4a和[Pt（DCA）（P）3]通过简单的快速路线从无机合成子[PtCO 3（Me 2 SO -S）2]，1制备作为中性配体的DCA，P = PPh 3 3b，P = PTA，4b）。确定了2、3、3a和4a的X射线晶体结构。评价了2，4a和4b对两种人癌细胞系顺铂敏感的A2780和顺铂耐药的SKOV-3的抗增殖活性，并将结果与​​已知的胺类似物和二氯化物前体进行了比较。