Influence of the Number of Axial Bexarotene Ligands on the Cytotoxicity of Pt(IV) Analogs of Oxaliplatin

轴向贝沙罗汀配体数量对奥沙利铂 Pt(IV) 类似物细胞毒性的影响

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作者:Yulia N Nosova, Ilia V Zenin, Varvara P Maximova, Ekaterina M Zhidkova, Kirill I Kirsanov, Ekaterina A Lesovaya, Anna A Lobas, Mikhail V Gorshkov, Olga N Kovaleva, Elena R Milaeva, Markus Galanski, Bernhard K Keppler, Alexey A Nazarov

Abstract

We present the synthesis and cytotoxic potencies of new Pt(IV) complexes with bexarotene, an anticancer drug that induces cell differentiation and apoptosis via selective activation of retinoid X receptors. In these complexes bexarotene is positioned as an axial ligand. The complex of one bexarotene ligand attached to Pt(IV) oxaliplatin moiety was potent whereas its counterpart carrying two bexarotene ligands was inactive.

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