Synthesis, antitumor activity, molecular modeling, and DNA binding properties of a new series of imidazonaphthalimides

被引:60
作者
Braña, MF
Cacho, M
García, MA
de Pascual-Teresa, B
Ramos, A
Acero, N
Llinares, F
Muñoz-Mingarro, D
Abradelo, C
Rey-Stolle, MF
Yuste, M
机构
[1] Univ San Pablo CEU, Fac Ciencias Expt & Salud, Dept Quim Organ, Madrid 28668, Spain
[2] Univ San Pablo CEU, Fac Ciencias Expt & Salud, Dept Biol, Madrid 28668, Spain
[3] Univ San Pablo CEU, Fac Ciencias Expt & Salud, Dept Ciencias Basicas, Madrid 28668, Spain
关键词
D O I
10.1021/jm020950q
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
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.
引用
收藏
页码:5813 / 5816
页数:4
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