Antitumor activity and COMPARE analysis of bis-indole derivatives

  • Bioorg Med Chem. 2010 May 1;18(9):3004-11. doi: 10.1016/j.bmc.2010.03.063.
Aldo Andreani  1 ,  Silvia Burnelli ,  Massimiliano Granaiola ,  Alberto Leoni ,  Alessandra Locatelli ,  Rita Morigi ,  Mirella Rambaldi ,  Lucilla Varoli ,  Laura Landi ,  Cecilia Prata ,  Francesco Vieceli Dalla Sega ,  Cristiana Caliceti ,  Robert H Shoemaker
Affiliations
  • 1. Dipartimento di Scienze Farmaceutiche, Università di Bologna, Via Belmeloro 6, 40126 Bologna, Italy. [email protected]
PMID: 20395150 DOI: 10.1016/j.bmc.2010.03.063
Abstract

This paper reports the synthesis of new derivatives (formed by two indole systems separated by a central moiety) analogous of potent antitumor agents previously described. The activity of the bis-indoles bearing a pyridine core confirms the good result described in the previous paper and compound 4c was chosen for the first in vivo experiment (Hollow Fiber Assay). COMPARE analysis and structure-activity relationships were also considered. Contrary to data reported by Other Authors, no correlations were found between antitumor activity and NQO1 induction.