Please use this identifier to cite or link to this item: http://hdl.handle.net/10397/8755
Title: Synthesis and evaluation of quindoline derivatives as G-quadruplex inducing and stabilizing ligands and potential inhibitors of telomerase
Authors: Zhou, JL
Lu, YJ
Ou, TM
Zhou, JM
Huang, ZS
Zhu, XF
Du, CJ
Bu, XZ
Ma, L
Gu, LQ
Li, YM
Chan, ASC
Issue Date: 2005
Source: Journal of medicinal chemistry, 2005, v. 48, no. 23, p. 7315-7321 How to cite?
Journal: Journal of Medicinal Chemistry 
Abstract: A new series of quindoline derivatives (4a-j) were designed and synthesized to develop novel and potent telomerase inhibitors. The interaction of the G-quadruplex of human telomere DNA with these newly designed molecules was examined via circular dichroism spectroscopy and electrophoretic mobility shift assay (EMSA). The selectivity between the quindoline derivative (4a) and G-quadruplex or duplex DNA was investigated by competition dialysis. These new compounds as inhibitors of telomerase were also investigated through the utilization of modified telomerase repeat amplification protocol (TRAP) assay. The results revealed that the introduction of electron-donating groups such as substituted amino groups at the C-11 position of quindoline significantly improved the inhibitory effect on telomerase activity ( TelIC 50 > 138 μM for quindoline, 0.44-12.3 μM for quindoline derivatives 4a-j). The quindoline derivatives not only stabilized the G-quadruplex structure but also induced the G-rich telomeric repeated DNA sequence to fold into quadruplex.
URI: http://hdl.handle.net/10397/8755
ISSN: 0022-2623
DOI: 10.1021/jm050041b
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