2. Academic Validation
  3. Synthesis, antitumor activity, molecular modeling, and DNA binding properties of a new series of imidazonaphthalimides

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

  • J Med Chem. 2002 Dec 19;45(26):5813-6. doi: 10.1021/jm020950q.
Miguel F Braña 1,  Mónica Cacho,  Mario A García,  Beatriz de Pascual-Teresa,  Ana Ramos,  Nuria Acero,  Francisco Llinares,  Dolores Muñoz-Mingarro,  Cristina Abradelo,  María Fernanda Rey-Stolle,  Mercedes Yuste
Affiliations

Affiliation

  • 1 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. [email protected]
PMID: 12477366 DOI: 10.1021/jm020950q
Abstract

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.

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