Nosova Yulia N, Zenin Ilia V, Maximova Varvara P, Zhidkova Ekaterina M, Kirsanov Kirill I, Lesovaya Ekaterina A, Lobas Anna A, Gorshkov Mikhail V, Kovaleva Olga N, Milaeva Elena R, Galanski Markus, Keppler Bernhard K, Nazarov Alexey A
Department of Medicinal Chemistry and Fine Organic Synthesis, Lomonosov Moscow State University, Leninskie Gory 1/3, Moscow 119991, Russia.
Blokhin Cancer Research Center, 24 Kashirskoye Shosse, Moscow 115478, Russia.
Bioinorg Chem Appl. 2017;2017:4736321. doi: 10.1155/2017/4736321. Epub 2017 Jul 19.
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.
我们展示了新型铂(IV)配合物与贝沙罗汀的合成及其细胞毒性效力,贝沙罗汀是一种抗癌药物,通过选择性激活视黄酸X受体诱导细胞分化和凋亡。在这些配合物中,贝沙罗汀作为轴向配体。一个贝沙罗汀配体连接到铂(IV)奥沙利铂部分的配合物具有活性,而携带两个贝沙罗汀配体的对应物则无活性。