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.
Andreani A., Burnelli S., Granaiola M., Leoni A., Locatelli A., Morigi R., et al. (2010). Antitumor activity and COMPARE analysis of bis-indole derivatives. BIOORGANIC & MEDICINAL CHEMISTRY, 18, 3004-3011 [10.1016/j.bmc.2010.03.063].
Antitumor activity and COMPARE analysis of bis-indole derivatives
ANDREANI, ALDO;BURNELLI, SILVIA;GRANAIOLA, MASSIMILIANO;LEONI, ALBERTO;LOCATELLI, ALESSANDRA;MORIGI, RITA;RAMBALDI, MIRELLA;VAROLI, LUCILLA;LANDI, LAURA;PRATA, CECILIA;CALICETI, CRISTIANA;
2010
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.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
