以非甾体抗炎药作为轴向配体的铂（IV）前药。
Pt(IV) Prodrugs with NSAIDs as Axial Ligands.
作者信息
Spector Daniil, Krasnovskaya Olga, Pavlov Kirill, Erofeev Alexander, Gorelkin Peter, Beloglazkina Elena, Majouga Alexander
机构信息
Department of Materials Science of Semiconductors and Dielectrics, National University of Science and Technology (MISIS), Leninskiy Prospect 4, 101000 Moscow, Russia.
Chemistry Department, Lomonosov Moscow State University, Leninskie Gory 1,3, 119991 Moscow, Russia.
出版信息
Int J Mol Sci. 2021 Apr 7;22(8):3817. doi: 10.3390/ijms22083817.
A chemo-anti-inflammatory strategy is of interest for the treatment of aggressive cancers. The platinum (IV) prodrug with non-steroidal anti-inflammatory drugs (NSAIDs) as axial ligands is designed to efficiently enter tumor cells due to high lipophilicity and release the cytotoxic metabolite and NSAID intracellularly, thereby reducing side effects and increasing the therapeutic efficacy of platinum chemotherapy. Over the last 7 years, a number of publications have been devoted to the design of such Pt(IV) prodrugs in combination with anti-inflammatory chemotherapy, with high therapeutic efficacy in vitro and In vivo. In this review, we summarize the studies devoted to the development of Pt(IV) prodrugs with NSAIDs as axial ligands, the study of the mechanism of their cytotoxic action and anti-inflammatory activity, the structure-activity ratio, and therapeutic efficacy.
一种化学抗炎策略对于侵袭性癌症的治疗具有重要意义。以非甾体抗炎药（NSAIDs）作为轴向配体的铂（IV）前药，因其高亲脂性而被设计用于有效进入肿瘤细胞，并在细胞内释放细胞毒性代谢物和NSAIDs，从而减少副作用并提高铂类化疗的治疗效果。在过去7年中，许多出版物致力于此类铂（IV）前药与抗炎化疗联合应用的设计，在体外和体内均具有高治疗效果。在本综述中，我们总结了有关以NSAIDs作为轴向配体的铂（IV）前药的开发研究、其细胞毒性作用和抗炎活性机制的研究、构效关系以及治疗效果。
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