Pt(II) complexes with different N-donor aromatic ligands for specific inhibition of telomerase

被引:35
作者
Cavigiolio, G
Benedetto, L
Boccaleri, E
Colangelo, D
Viano, I
Osella, D
机构
[1] Univ Piemonte Orientale, Dipartimento Sci & Tecnol Avanzate, I-15100 Alessandria, Italy
[2] Univ Piemonte Orientale, Dipartimento Sci Med, I-15100 Alessandria, Italy
[3] Univ Turin, Dipartimento Chim, IFM, I-10125 Turin, Italy
关键词
antitumor agents; platinum complexes; isoquinoline complexes; telomerase;
D O I
10.1016/S0020-1693(00)00114-6
中图分类号
O61 [无机化学];
学科分类号
070301 ; 081704 ;
摘要
A number of cis-dichloroplatinum(II) derivatives containing aromatic N-donor ligands such as pyridine and/or 5-substituted isoquinolines have been synthesized and fully characterized, with particular use of Raman spectroscopy and mass spectrometry. These complexes have been tested for specific inhibition of telomerase, which could represent a selective target for cancer chemotherapy. The screening of such potential drugs has been performed by a biochemical assay on the isolated enzyme, It is noteworthy that the cis -[PtCl2(pyridine)(5-SO3H-isoquinoline)] compound exhibited remarkable telomerase inhibition at a concentration as low as 10(-7) M. (C) 2000 Elsevier Science S.A. All rights reserved.
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页码:61 / 68
页数:8
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