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首页> 外文期刊>Journal of Medicinal Chemistry >Interactions of platinum complexes containing cationic, bicyclic, nonplanar piperidinopiperidine ligands with biological nucleophiles
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Interactions of platinum complexes containing cationic, bicyclic, nonplanar piperidinopiperidine ligands with biological nucleophiles

机译：含阳离子，双环，非平面哌啶子基哌啶配体的铂配合物与生物亲核试剂的相互作用

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摘要

The determination of the structures and DNA interactions and the reactions with GSH and ubiquitin of complexes of the general formula trans-[PtCl2(Am)(pip-pip)]center dot HCl, where pip-pip is 4-piperidinopiperidine and Am is NH3, methylamine (MA), dimethylamine (DMA), n-propylamine (NPA), isopropylamine (IPA), n-butylamine (NBA), or cyclohexylamine (CHA), were performed. X-ray structures and NMR studies of the NH3 and MA complexes showed that both pip rings were in the chair conformation and that the second pip ring is fluxional. The DNA binding studies showed that these complexes bind to calf thymus DNA nearly an order of magnitutde more quickly than cisplatin and form covalent adducts that stabilize the double helix. The binding of the pip- pip complexes to DNA results in high unwinding angles (similar to 30 degrees) and in the formation of similar to 25% interstrand cross-links. The pip-pip complexes reacted with GSH more quickly than cisplatin and transplatin, and the rate of reaction decreased with increasing steric bulk of the ligand trans to the pip-pip. The reactions with ubiquitin resulted in monofunctional binding to Met1. Only the NH3, MA, and DMA complexes reacted with ubiquitin in a slower and less efficient fashion than cisplatin.
机译：通式反式[[PtCl2（Am）（pip-pip）]中心点HCl，其中pip-pip为4-piperidinopiperidine，Am为NH3）的配合物的结构和DNA相互作用以及与GSH和泛素的反应的测定进行了甲胺（MA），二甲胺（DMA），正丙胺（NPA），异丙胺（IPA），正丁胺（NBA）或环己胺（CHA）的检测。 NH3和MA配合物的X射线结构和NMR研究表明，两个pip环均处于椅子构象，第二个pip环是可通量的。 DNA结合研究表明，这些复合物与小牛胸腺DNA的结合速度比顺铂快近一个数量级，可形成稳定双螺旋的共价加合物。 pip-pip复合物与DNA的结合导致高解链角（大约30度）并形成大约25％的链间交联。 pip-pip复合物与GSH的反应比顺铂和反铂更快，并且反应速率随着配体向pip-pip立体位阻的增加而降低。与泛素的反应导致与Met1的单功能结合。只有NH3，MA和DMA复合物与泛素的反应比顺铂更慢，效率更低。

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