NITRACRINE AND ITS CONGENERS - AN OVERVIEW

被引:39
作者
GNIAZDOWSKI, M
SZMIGIERO, L
机构
来源
GENERAL PHARMACOLOGY | 1995年 / 26卷 / 03期
关键词
NITRACRINE; ACRIDINES; BISACRIDINES; ANTICANCER DRUGS; CYTOSTATICS; DNA INTERACTING LIGANDS;
D O I
10.1016/0306-3623(94)00143-B
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
1. An anticancer drug, nitracrine 1-nitro-9(3'3'-dimethylaminopropylamino)acridine (Ledakrin, C-283) exhibits potent cytostatic effects which can be ascribed to interactions of the drug with DNA. 2. The reduction of the nitro group of nitracrine is one of the activation steps leading to the drug covalent binding to DNA and proteins both in subcellular systems and in the cell. 3. DNA-drug non-covalent interactions and covalent complexes are examined in several model systems and compared with the properties of a number of derivatives with programmed structural changes. 4. DNA-protein crosslinks and interstrand crosslinks are detected in the cells following exposition to the drug. 5. The drug exhibits selective toxicity and radiosensitization effects to hypoxic mammalian cells.
引用
收藏
页码:473 / 481
页数:9
相关论文
共 67 条
[1]  
Acheson, Taylor, Waring, Haylock, Abel, The intercalative DNA binding and antitumor activity of some bis-acridines related to nitracrine, Chem.-Biol. Interact., 53, pp. 371-375, (1985)
[2]  
Anderson, Denny, Roberts, Wardman, White, Wilson, Correlation of the radiosenzitization potency afforded by nitroacridine intercalators with their electron scavenging efficiency in DNA, Int. J. Radiat. Oncol. Biol. Phys., 22, pp. 537-540, (1992)
[3]  
Baguley, DNA intercalating anti-tumour agents, Anti-Cancer Drug Des., 6, pp. 1-35, (1991)
[4]  
Bartoszek, Konopa, <sup>32</sup>P-post-labeling analysis of DNA adducts formation by antitumor drug Nitracrine and other nitroacridines in different biological systems, Biochem. Pharmac., 38, pp. 1301-1312, (1989)
[5]  
Bartoszek, Skladanowski, A quantative analysis of cytotoxic action of some 1-nitro-9-amino-acridines against HeLa S<sub>3</sub> cells, J. Cell Pharmac., 2, pp. 305-310, (1991)
[6]  
Boyd, Denny, NMR studies of configuration and tautomeric equilibria in nitroacridine antitumor agents, J. med. Chem., 33, pp. 2656-2659, (1990)
[7]  
Bratkowska-Seniow, Dziedzic, Fengler, Steuden, Szymaniec, Wysocka, Morphologic blood pathern in patients treated with Ledakrin, Mater Med Pol, 8, pp. 295-301, (1976)
[8]  
Bratkowska-Seniow, Oleszkiewicz, Kozak, Krizar, Ledakrin in treatment of colon carcinoma, Mater Med Pol, 8, pp. 323-330, (1976)
[9]  
Chodkowski, Kiwak, Polarographic investigations on acridine derivatives. Part V. 1-nitro-9-alkyl-aminoacridines, Roczniki Chem., 47, pp. 1401-1408, (1973)
[10]  
Ciesielska, Piestrzeniewicz, Galasinski, Gniazdowski, Properties of nitracrine-nucleic acids complexes in selected enzymatic systems, Acta Univ. Lodz. Folia Biochem. Biophys., 6, pp. 73-81, (1988)