Synthesis, cytotoxicity and apoptosis of cyclotriphosphazene compounds as anti-cancer agents

被引:97
作者
Yildirim, Tuba [1 ]
Bilgin, Kemal [2 ]
Ciftci, Gonul Yenilmez [3 ]
Ecik, Esra Tanriverdi [3 ]
Senkuytu, Elif [3 ]
Uludag, Yildiz [4 ]
Tomak, Leman [5 ]
Kilic, Adem [3 ]
机构
[1] Amasya Univ, Dept Biol, Fac Art & Sci, TR-05100 Amasya, Turkey
[2] Ondokuz Mayis Univ, Dept Med Microbiol, Fac Med, TR-55139 Samsun, Turkey
[3] Gebze Inst Technol, Dept Chem, TR-41400 Gebze, Turkey
[4] UEKAE Sci & Technol Res Council Turkey TUBITAK, TR-41470 Gebze, Turkey
[5] Ondokuz Mayis Univ, Dept Biostat, Fac Med, TR-55139 Samsun, Turkey
关键词
Cyclotriphosphazene; Spermine derivatives; Biological activity; Cytotoxic activity; Apoptosis; CONFORMATIONALLY RESTRICTED ANALOGS; ANTIBIOTIC SUSCEPTIBILITY; SPERMINE; POLYAMINES; GROWTH; CYCLOPHOSPHAZENES; POLYPHOSPHAZENE; DERIVATIVES; BINDING;
D O I
10.1016/j.ejmech.2012.03.018
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
In the present study, a number of new dispirobino and dispiroansa spermine derivatives of cyclotriphosphazene (8-10, 13) were synthesized and characterized by elemental analysis, mass spectrometry, H-1 and P-31 NMR spectroscopy. At first, in vitro cytotoxic activity of cyclotriphosphazene compounds (1-14) against HT-29 (human colon adenocarcinoma), Hep2 (Human epidermoid larynx carcinoma), and Vero (African green monkey kidney) cell lines was investigated. Our study showed that most of these compounds stimulate apoptosis and they have cytotoxic effects for HT-29 and Hep2 cells. Additionally, these compounds (1-14) were investigated for their antibacterial activity against gram-positive (Staphylococcus aureus), gram-negative (Escherichia coli, Pseudomonas aeruginosa) bacteria and for their antifungal activity against Candida albicans, and were shown to be inactive. (C) 2012 Elsevier Masson SAS. All rights reserved.
引用
收藏
页码:213 / 220
页数:8
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