A novel inhibitor of human telomerase derived from 10H-indolo [3, 2-b] quinoline

V Caprio, B Guyen, Y Opoku-Boahen, J Mann…

文献索引：Caprio, Vittorio; Guyen, Berengere; Opoku-Boahen, Yaw; Mann, John; Gowan, Sharon M.; Kelland, Lloyd M.; Read, Martin A.; Neidle, Stephen Bioorganic and Medicinal Chemistry Letters, 2000 , vol. 10, # 18 p. 2063 - 2066

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被引用次数: 109

摘要

The bis-dimethylaminoethyl derivative of quindoline (10H-indolo [3, 2-b] quinoline), an alkaloid from the West African shrub Cryptolepis sanguinolenta, has been synthesised. This has been shown to have modest cytotoxicity, as well as inhibitory activity against the telomerase enzyme. It is hypothesised that the latter activity is due to stabilisation of an intermediate guanine-quadruplex complex, in accordance with computer modelling.