2. Academic Validation
  3. Antitumor activity and COMPARE analysis of bis-indole derivatives

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

Affiliation

  • 1 Dipartimento di Scienze Farmaceutiche, Università di Bologna, Via Belmeloro 6, 40126 Bologna, Italy. aldo.andreani@unibo.it
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.

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