Rational design of acridine-based ligands with selectivity for human telomeric quadruplexes

…, SM Haider, F Doria, M Gunaratnam…

Index: Sparapani, Silvia; Haider, Shozeb M.; Doria, Filippo; Gunaratnam, Mekala; Neidle, Stephen Journal of the American Chemical Society, 2010 , vol. 132, # 35 p. 12263 - 12272

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Citation Number: 71

Abstract

Structure-based modeling methods have been used to design a series of disubstituted triazole-linked acridine compounds with selectivity for human telomeric quadruplex DNAs. A focused library of these compounds was prepared using click chemistry and the selectivity concept was validated against two promoter quadruplexes from the c-kit gene with known molecular structures, as well as with duplex DNA using a FRET-based melting method. ...