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一种安全有效的 Pt(ii)抗癌前药:设计、合成、体外疗效、载体配体的作用和体内肿瘤生长抑制。

A safe and efficacious Pt(ii) anticancer prodrug: design, synthesis, in vitro efficacy, the role of carrier ligands and in vivo tumour growth inhibition.

机构信息

Invictus Oncology Pvt. Ltd., 465 Patparganj Industrial Area, Delhi 110092, India.

出版信息

Chem Commun (Camb). 2019 Feb 5;55(12):1718-1721. doi: 10.1039/c8cc06586a.

Abstract

Diaminocyclohexane-Pt(ii)-phenalenyl complexes (1 and 2) showed an appropriate balance between efficacy and toxicity. Compound 2 showed nearly two-fold higher tumour growth inhibition than oxaliplatin in a murine NSCLC tumour model, when a combined drug development approach was used. The fluorescent properties of phenalenone were utilized to understand the mechanistic details of the drug.

摘要

二胺环己烷-Pt(ii)-菲咯啉配合物(1 和 2)在疗效和毒性之间表现出适当的平衡。当采用联合药物开发方法时,化合物 2 在小鼠 NSCLC 肿瘤模型中显示出比奥沙利铂高近两倍的肿瘤生长抑制作用。菲咯酮的荧光性质被用于了解药物的机制细节。

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