新型甲硅烷基和三苯甲基修饰核苷的合成及其体外生长抑制活性
Synthesis and in vitro growth inhibitory activity of novel silyl- and trityl-modified nucleosides.
作者信息
Panayides Jenny-Lee, Mathieu Véronique, Banuls Laetitia Moreno Y, Apostolellis Helen, Dahan-Farkas Nurit, Davids Hajierah, Harmse Leonie, Rey M E Christine, Green Ivan R, Pelly Stephen C, Kiss Robert, Kornienko Alexander, van Otterlo Willem A L
机构信息
Molecular Sciences Institute, School of Chemistry, University of the Witwatersrand, PO Wits, Johannesburg 2050, South Africa; Pioneering Health Sciences, CSIR Biosciences, PO Box 395, Pretoria 0001, South Africa.
Laboratoire de Cancérologie et de Toxicologie Expérimentale, Faculté de Pharmacie, Université Libre de Bruxelles, Brussels, Belgium.
出版信息
Bioorg Med Chem. 2016 Jun 15;24(12):2716-24. doi: 10.1016/j.bmc.2016.04.036. Epub 2016 Apr 20.
Seventeen silyl- and trityl-modified (5'-O- and 3',5'-di-O-) nucleosides were synthesized with the aim of investigating the in vitro antiproliferative activities of these nucleoside derivatives. A subset of the compounds was evaluated at a fixed concentration of 100μM against a small panel of tumor cell lines (HL-60, K-562, Jurkat, Caco-2 and HT-29). The entire set was also tested at varying concentrations against two human glioma lines (U373 and Hs683) to obtain GI50 values, with the best results being values of ∼25μM.
合成了17种硅烷基和三苯甲基修饰的（5'-O-和3',5'-二-O-）核苷，目的是研究这些核苷衍生物的体外抗增殖活性。以100μM的固定浓度对一小部分肿瘤细胞系（HL-60、K-562、Jurkat、Caco-2和HT-29）评估了该化合物子集。还以不同浓度对两个人胶质瘤细胞系（U373和Hs683）测试了整个化合物集，以获得GI50值，最佳结果为约25μM。
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