Trisubstituted acridine derivatives as potent and selective telomerase inhibitors

RJ Harrison, J Cuesta, G Chessari…

Index: Harrison, R. John; Cuesta, Javier; Chessari, Gianni; Read, Martin A.; Basra, Sanji K.; Reszka, Anthony P.; Morrell, James; Gowan, Sharon M.; Incles, Christopher M.; Tanious, Farial A.; Wilson, W. David; Kelland, Lloyd R.; Neidle, Stephen Journal of Medicinal Chemistry, 2003 , vol. 46, # 21 p. 4463 - 4476

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Citation Number: 165

Abstract

The synthesis and evaluation for telomerase-inhibitory and quadruplex DNA binding properties of three related series of rationally designed trisubstituted acridine derivatives are described. These are substituted on the acridine ring at the 2, 6, 9; 2, 7, 9; and 3, 6, 9 positions. The ability of several of the most potent compounds to interact with and stabilize an intramolecular G-quadruplex DNA was evaluated by surface plasmon resonance ...