Gold(I) complexes with alkylated PTA (1,3,5-triaza-7-phosphaadamantane) phosphanes as anticancer metallodrugs

被引：40

作者：

Garcia-Moreno, Elena ^{[1
]}

Gascon, Sonia ^{[2
]}

Atrian-Blasco, Elena ^{[1
]}

Jesus Rodriguez-Yoldi, Ma ^{[2
]}

Cerrada, Elena ^{[1
]}

Laguna, Mariano ^{[1
]}

机构：

[1] Univ Zaragoza, CSIC, Inst Sintesis Quim & Catalisis Homogenea, Dept Quim Inorgan, E-50009 Zaragoza, Spain

[2] Univ Zaragoza, Fac Vet, Unidad Fisiol, Dept Farmacol & Fisiol,CIBERobn, E-50013 Zaragoza, Spain

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2014年 / 79卷

关键词：

Gold; Thiolate; Water soluble; PTA; Antitumor properties; THIOREDOXIN REDUCTASE INHIBITION; METAL-BASED CHEMOTHERAPY; IN-VITRO CYTOTOXICITY; ANTITUMOR-ACTIVITY; PHOSPHINE COMPLEXES; COORDINATION-COMPLEXES; RHEUMATOID-ARTHRITIS; THERAPEUTIC AGENTS; CARBENE COMPLEXES; TROPICAL DISEASES;

D O I：

10.1016/j.ejmech.2014.04.001

中图分类号：

R914 [药物化学];

学科分类号：

100705 [微生物与生化药学];

摘要：

New stable thiolate gold(I) derivatives containing the alkylated phosphanes [PTA-CH2Ph]Br and [PTA -CH2COOMe]Br derived from 1,3,5-triaza-7-phosphaadamantane (PTA) have been prepared by different routes of synthesis. By the use of basic media to deprotonate the corresponding thiol in the former and by transmetallation reactions from tin (IV) complexes, in the later, thus avoiding side reactions on the phosphane. Strong antiproliferative effects are observed for most of the compounds, including the chloro-and bromo precursors with the series of phosphanes derived from PTA, in human colon cancer cell lines (Caco-2, PD7 and TC7 clones). Apoptosis-induced cell death is found for all compounds, being the thiolate derivatives with [PTA-CH2Ph]Br the most effective, as shown by an annexin-V/propidium iodide double-staining assay. (c) 2014 Elsevier Masson SAS. All rights reserved.

引用

页码：164 / 172

页数：9

共 64 条

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