Solid-phase synthesis and pharmacological evaluation of novel nucleoside-tethered dinuclear platinum(II) complexes

被引：15

作者：

D'Errico, Stefano ^{[1
]}

Oliviero, Giorgia ^{[1
]}

Piccialli, Vincenzo ^{[2
]}

Amato, Jussara ^{[1
]}

Borbone, Nicola ^{[1
]}

D'Atri, Valentina ^{[1
]}

D'Alessio, Francesca ^{[3
]}

Di Noto, Rosa ^{[3
,4
]}

Ruffo, Francesco ^{[5
]}

Salvatore, Francesco ^{[3
,6
]}

Piccialli, Gennaro ^{[1
]}

机构：

[1] Univ Naples Federico II, Dipartimento Chim Sostanze Nat, I-80131 Naples, Italy

[2] Univ Naples Federico II, Dipartimento Chim Organ & Biochim, I-80126 Naples, Italy

[3] CEINGE Biotecnol Avanzate, I-80145 Naples, Italy

[4] Univ Naples Federico II, Dipartimento Biochim & Biotecnol Med, I-80131 Naples, Italy

[5] Univ Naples Federico II, Dipartimento Chim, I-80126 Naples, Italy

[6] IRCCS Fdn SDN, Naples, Italy

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2011年 / 21卷 / 19期

关键词：

Dinuclear platinum complexes; Nucleosides; Solid-phase synthesis; Anti-tumor compounds; DNA-BINDING; CISPLATIN RESISTANCE; ANTITUMOR-ACTIVITY; RIBOSE; N,N'-BIS(AMINOALKYL)-1,4-DIAMINOANTHRAQUINONES; CYTOTOXICITY; MECHANISM; LIGANDS; ANALOGS; CARRIER;

D O I：

10.1016/j.bmcl.2011.07.104

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Three novel inosine-based dinuclear platinum complexes have been synthesized via a solid-phase strategy. In these compounds, the metal is linked both to the N-7 of the purine nucleus and to the terminal amine group of a hexylamine side chain installed on N-1. Cis- or trans- diamine as well as ethylenediamine ligands are coordinated to platinum along with a chloride. The synthesised complexes were tested against four different human tumor cell lines. One of these complexes proved to be more cytotoxic than cisplatin against the MCF7 cancer cell line in a short-term exposure assay. (C) 2011 Elsevier Ltd. All rights reserved.

引用

页码：5835 / 5838

页数：4

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