Non-classical anticancer agents: synthesis and biological evaluation of zinc(II) heteroleptic complexes

被引：84

作者：

Liguori, Paola F. ^{[2
]}

Valentini, Alessandra ^{[3
,4
]}

Palma, Mariagrazia ^{[5
]}

Bellusci, Anna ^{[2
]}

Bernardini, Sergio ^{[3
,4
]}

Ghedini, Mauro ^{[2
]}

Panno, Maria Luisa ^{[5
]}

Pettinari, Claudio ^{[6
]}

Marchetti, Fabio ^{[6
]}

Crispini, Alessandra ^{[1
]}

Pucci, Daniela ^{[2
]}

机构：

[1] Univ Calabria, Dipartimento Sci Farmaceut, CR INSTM Unita Calabria, Ctr Eccellenza CEMIF CAL LASCAMM, I-87030 Commenda Di Rende, Italy

[2] Univ Calabria, Dipartimento Chim, CR INSTM Unita Calabria, Ctr Eccellenza CEMIF CAL LASCAMM, I-87030 Commenda Di Rende, Italy

[3] Univ Roma Tor Vergata, PTV, Dept Lab Med, Rome, Italy

[4] Univ Roma Tor Vergata, PTV, Dept Internal Med, Rome, Italy

[5] Univ Calabria, Dipartimento Biol Cellulare, I-87030 Arcavacata Di Rende, CS, Italy

[6] Univ Camerino, Dipartimento Sci Chim, I-62032 Camerino, Italy

来源：

DALTON TRANSACTIONS | 2010年 / 39卷 / 17期

关键词：

PROSTATE-CANCER CELLS; X-RAY STRUCTURES; METAL-COMPLEXES; DNA-BINDING; COORDINATION CHEMISTRY; CYTOTOXIC ACTIVITY; ANTITUMOR-ACTIVITY; INDUCED APOPTOSIS; BETA-THUJAPLICIN; ZN(II) COMPLEXES;

D O I：

10.1039/b922101h

中图分类号：

O61 [无机化学];

学科分类号：

070301 ; 081704 ;

摘要：

New heteroleptic complexes (1-8) containing Zn(II) ion coordinated to an N, N-chelating ligand (the 4,4'-dinonyl-2,2'-bipyridine, bpy-9) and to diketonates L such as tropoloids (Tropolone and Hinokitiol) or 1-phenyl-3-methyl-4-R-5-pyrazolones have been synthesized by using different stoichiometric ratio with respect to the L ancillary ligand. The molecular structure of the bis-tropolonate derivative [(bpy-9) Zn(L)(2)] 5 has been determined by single-crystal X-ray diffraction. The antitumour activity of all Zn(II) complexes was tested in vitro against three different human prostate cancer cells: DU145, LNCaP and PC-3. Moreover, their effect on cell survival signalling and/or inhibitors of the PC-3 cell cycle have been analyzed. The results indicate that 1-8 exhibit strong cytotoxic activity against all cell lines affecting key molecules such as p-AKT and p21 waf, involved in the cell proliferation and/or arrest. Zinc(II) is thus a promising alternative to Pt(II) ion in the design of new, better performing antitumour agents.

引用

页码：4205 / 4212

页数：8

共 61 条

[1] Zinc metalloproteins as medicinal targets [J].