新型单萘二甲酰亚胺和双萘二甲酰亚胺的合成、生物学评价及DNA结合特性
Synthesis, biological evaluation and DNA binding properties of novel mono and bisnaphthalimides.
作者信息
Braña Miguel F, Cacho Mónica, Ramos Ana, Domínguez M Teresa, Pozuelo Jose M, Abradelo Cristina, Rey-Stolle M Fernanda, Yuste Mercedes, Carrasco Carolina, Bailly Christian
机构信息
Departamento de CC. Químicas, Facultad de CC. Experimentales y de la Salud, Universidad San Pablo CEU, Urb. Montepríncipe, Boadilla del Monte, 28668 Madrid, Spain.
出版信息
Org Biomol Chem. 2003 Feb 21;1(4):648-54. doi: 10.1039/b209042b.
A novel series of mono and bisnaphthalimides was synthesized and their antiproliferative activities were evaluated against three tumor cell lines. Bisnaphthalimides 3 and 4, bearing a pyrazine ring fused to the naphthalimide system, showed activities in the order of 10(-8) microM, similar to elinafide. DNA binding properties and the ability to induce DNA damage were studied for some of the most active compounds.
合成了一系列新型的单萘二甲酰亚胺和双萘二甲酰亚胺，并评估了它们对三种肿瘤细胞系的抗增殖活性。带有与萘二甲酰亚胺体系稠合的吡嗪环的双萘二甲酰亚胺3和4，其活性顺序为10(-8) microM，与依利萘德相似。对一些活性最强的化合物研究了其DNA结合特性和诱导DNA损伤的能力。
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