Synthesis, biological activity, and quantitative structure-activity relationship study of azanaphthalimide and arylnaphthalimide derivatives

  • J Med Chem. 2004 Apr 22;47(9):2236-42. doi: 10.1021/jm0310784.
Miguel F Braña  1 ,  Ana Gradillas ,  Angel Gómez ,  Nuria Acero ,  Francisco Llinares ,  Dolores Muñoz-Mingarro ,  Cristina Abradelo ,  Fernanda Rey-Stolle ,  Mercedes Yuste ,  Joaquín Campos ,  Miguel A Gallo ,  Antonio Espinosa
Affiliations
  • 1. Departamento de Ciencias Químicas, Universidad San Pablo CEU, Urbanización Montepríncipe, 28668-Boadilla del Monte, Madrid, Spain. [email protected]
Abstract

A series of quinoline derivatives as aza analogues of the naphthalene chromophore and a series of "nonfused" tricyclic aromatic systems, in particular 5-arylquinolines and 5- or 6-aryl and heteroaryl naphthalene systems, were synthesized and evaluated for growth-inhibitory properties in several human cell lines. The analysis of quantitative structure-antitumor activity relationships for the growth-inhibitory properties is also reported. Findings suggest that these compounds may not express their cytotoxicity via interaction on DNA.