Structure and Unique Interactions with DNA of a Cationic <i>Trans</i>‐Platinum Complex with the Nonplanar Bicyclic Piperidinopiperidine Ligand

Yousef Najajreh, Dmitri Prilutski, Yael Ardeli‐Tzaraf, Jose M. Pérez, Elena Khazanov, Yechezkel Barenholz, Jana Kašpárková, Viktor Brabec, Dan Gibson

Angewandte Chemie International Edition · 2005 · 35 citations · 13 references

Concepts

Abstract

Circumventing cisplatin resistance: The trans-[PtCl2(NH3)(pip-pip)]+ ion (see structure; red Pt, blue N, green Cl, gray C) is a cytotoxic compound with a cationic piperidinopiperidine ligand. The piperidine ring that is removed from the PtII center is fluxional and acts as a hydrogen-bond donor. The complex binds calf thymus DNA directly and rapidly (t1/2=11 min) without prior hydrolysis and circumvents cisplatin resistance in ovarian cancer cells.

References

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