新型咪唑并萘二甲酰亚胺系列的合成、抗肿瘤活性、分子模拟及DNA结合特性
Synthesis, antitumor activity, molecular modeling, and DNA binding properties of a new series of imidazonaphthalimides.
作者信息
Braña Miguel F, Cacho Mónica, García Mario A, de Pascual-Teresa Beatriz, Ramos Ana, Acero Nuria, Llinares Francisco, Muñoz-Mingarro Dolores, Abradelo Cristina, Rey-Stolle María Fernanda, Yuste Mercedes
机构信息
Departamentos de Química Orgánica y Farmacéutica, Facultad de Ciencias Experimentales y de la Salud, Universidad San Pablo CEU, Urbanización Montepríncipe, 28668-Boadilla del Monte, Madrid, Spain.
出版信息
J Med Chem. 2002 Dec 19;45(26):5813-6. doi: 10.1021/jm020950q.
A series of mono and bisintercalators based on the 5,8-dihydrobenz[de]imidazo[4,5-g]isoquinoline-4,6-dione system were synthesized and evaluated for growth inhibitory properties in several human cell lines. All target compounds showed activity in the micromolar range. Representative compounds were evaluated using UV--vis spectroscopy and viscosimetric determinations, showing that they behave as DNA intercalators. Molecular modeling techniques were used in order to rationalize the moderate activity observed for bisnaphthalimides.
合成了一系列基于5,8 - 二氢苯并[de]咪唑并[4,5 - g]异喹啉 - 4,6 - 二酮体系的单插入剂和双插入剂，并在几种人类细胞系中评估了它们的生长抑制特性。所有目标化合物在微摩尔范围内均表现出活性。使用紫外 - 可见光谱和粘度测定法对代表性化合物进行了评估，结果表明它们表现为DNA插入剂。为了合理解释双萘二甲酰胺观察到的中等活性，使用了分子建模技术。
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