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烟酰胺配位的铂(IV)-钌(II)嵌合配合物在体内具有协同抑制肿瘤转移和生长的作用,同时潜在降低毒性。

Niacin-ligated platinum(iv)-ruthenium(ii) chimeric complexes synergistically suppress tumor metastasis and growth with potentially reduced toxicity in vivo.

机构信息

The First Affiliated Hospital, Key Laboratory of Combined Multi-Organ Transplantation, Ministry of Public Health, School of Medicine, Zhejiang University, Hangzhou, 310003, P. R. China.

Department of Medical Oncology, Sir Run Run Shaw Hospital, School of Medicine, Zhejiang University, Hangzhou, 310016, P. R. China.

出版信息

Chem Commun (Camb). 2020 Mar 10;56(20):3069-3072. doi: 10.1039/c9cc09016a.

Abstract

Niacin-ligated platinum(iv)-ruthenium(ii) chimeric complexes (PtRu 1-4) have been synthesized and evaluated for their antitumor performance. Using the optimal complex, PtRu-1, we show that this water-soluble chimeric prodrug not only potently inhibits the metastasis and proliferation of tumor cells but also has an unexpectedly higher safety margin in animals compared with the traditionally-used, clinically approved drug cisplatin.

摘要

已合成烟酸连接的铂(IV)-钌(II)嵌合配合物(PtRu1-4),并对其抗肿瘤性能进行了评估。使用最佳配合物 PtRu-1,我们表明这种水溶性嵌合前药不仅能强烈抑制肿瘤细胞的转移和增殖,而且与传统的临床批准药物顺铂相比,在动物体内具有出人意料的更高安全性。

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