作为抗癌剂的环三磷腈化合物的合成、细胞毒性和细胞凋亡。
Synthesis, cytotoxicity and apoptosis of cyclotriphosphazene compounds as anti-cancer agents.
机构信息
Department of Biology, Faculty of Art and Science, Amasya University, 05100 Amasya, Turkey.
出版信息
Eur J Med Chem. 2012 Jun;52:213-20. doi: 10.1016/j.ejmech.2012.03.018. Epub 2012 Mar 19.
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, (1)H and (31)P 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.
在本研究中，合成了一系列新的二吡咯并[3,2-f：3′,2′-h]吡咯并[1,2-a]氮丙啶和二吡咯并[3,2-f：3′,2′-h]吡咯并[1,2-a]三亚甲胺螺环磷腈衍生物（8-10、13），并通过元素分析、质谱、（1）H 和（31）P NMR 光谱进行了表征。首先，研究了环三磷腈化合物（1-14）对 HT-29（人结肠腺癌）、Hep2（人表皮样喉癌）和 Vero（非洲绿猴肾）细胞系的体外细胞毒性活性。我们的研究表明，这些化合物大多数都能刺激细胞凋亡，对 HT-29 和 Hep2 细胞具有细胞毒性作用。此外，还研究了这些化合物（1-14）对革兰氏阳性（金黄色葡萄球菌）、革兰氏阴性（大肠杆菌、铜绿假单胞菌）细菌的抗菌活性和对白色念珠菌的抗真菌活性，结果显示它们没有活性。
Zotero 插件