Synthesis and evaluation of analogues of 10H-indolo [3, 2-b] quinoline as G-quadruplex stabilising ligands and potential inhibitors of the enzyme telomerase

B Guyen, CM Schultes, P Hazel, J Mann…

Index: Guyen, Berangere; Schultes, Christoph M.; Hazel, Pascale; Mann, John; Neidle, Stephen Organic and Biomolecular Chemistry, 2004 , vol. 2, # 7 p. 981 - 988

Full Text: HTML

Citation Number: 107

Abstract

We report here the synthesis and evaluation for telomerase-inhibitory and quadruplex DNA binding properties of several rationally-designed quindoline analogues, substituted at the 2- and 7-positions. The ability of these compounds to interact with and stabilise an intramolecular G-quadruplex DNA against increases in temperature was evaluated by a fluorescence-based (FRET) melting assay. The resulting Tm values were found to ...