Journal
ACS MEDICINAL CHEMISTRY LETTERS
Volume 1, Issue 7, Pages 306-310Publisher
AMER CHEMICAL SOC
DOI: 10.1021/ml100062z
Keywords
DNA; quadruplex; c-kit regulation; inhibition; ligand
Categories
Funding
- BBSRC
- Cancer Research UK
- National Institutes of Health [1P50CAI27003-03]
- GI SPORE [1P50CAI27003-04]
- BBSRC [BB/E012752/1] Funding Source: UKRI
- Biotechnology and Biological Sciences Research Council [BB/E012752/1] Funding Source: researchfish
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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.
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