Bejugam, M., Gunaratnam, M., Müller, S., Sanders, D.A., Sewitz, S., Fletcher, J.A., Neidle, S. and Balasubramanian, S. (2010) Targeting thec-KitPromoter G-quadruplexes with 6-Substituted Indenoisoquinolines. ACS Medicinal Chemistry Letters, 1 (7). pp. 306-310.
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Herein, we demonstrate the design, synthesis, biophysical properties, and preliminary biological evaluation of 6-substituted indenoisoquinolines as a new class of G-quadruplex stabilizing small molecule ligands. We have synthesized 6-substituted indenoisoquinolines 1a-e in two steps from commercially available starting materials with excellent yields. The G-quadruplex stabilization potential of indenoisoquinolines 1a-e was evaluated by fluorescence resonance energy transfer-melting analysis, which showed that indenoisoquinolines show a high level of stabilization of various G-quadruplex DNA structures. Indenoisoquinolines demonstrated potent inhibition of cell growth in the GIST882 patient-derived gastrointestinal stromal tumor cell line, accompanied by inhibition of both c-Kit transcription and KIT oncoprotein levels
|Uncontrolled Keywords:||c-kit regulation; DNA; inhibition; ligand; quadruplex|
|Departments, units and centres:||Department of Pharmaceutical and Biological Chemistry > Department of Pharmaceutical and Biological Chemistry|
|Journal or Publication Title:||ACS Medicinal Chemistry Letters|
|Deposited By:||Library Staff|
|Deposited On:||20 Jan 2012 14:28|
|Last Modified:||20 Jan 2012 14:28|
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