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Influence of the Number of Axial Bexarotene Ligands on the Cytotoxicity of Pt(IV) Analogs of Oxaliplatin.
Bioinorganic Chemistry and Applications ( IF 3.8 ) Pub Date : 2017-07-19 , DOI: 10.1155/2017/4736321
Yulia N Nosova 1 , Ilia V Zenin 1 , Varvara P Maximova 2 , Ekaterina M Zhidkova 2 , Kirill I Kirsanov 2 , Ekaterina A Lesovaya 2 , Anna A Lobas 3 , Mikhail V Gorshkov 3 , Olga N Kovaleva 4 , Elena R Milaeva 1 , Markus Galanski 5 , Bernhard K Keppler 5 , Alexey A Nazarov 1
Affiliation  

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.

中文翻译:

轴性比沙罗汀烯配体数目对奥沙利铂Pt(IV)类似物的细胞毒性的影响。

我们介绍了新的Pt(IV)与贝沙罗汀的复合物的合成和细胞毒性,贝沙罗汀是一种抗癌药,通过选择性激活类维生素A X受体诱导细胞分化和凋亡。在这些配合物中,贝沙罗汀被定位为轴向配体。与Pt(IV)奥沙利铂部分连接的一个贝沙罗汀配体的复合物有效,而带有两个贝沙罗汀配体的对应物则没有活性。
更新日期:2017-07-19
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