Tsotinis, A., Vlachou, M., Zouroudis, S., Jeney, A., Timar, F., Thurston, D.E. and Roussakis, C. (2005) A Facile Synthesis of C2-Substituted Pyrrolo[2,3-f]quinolines with Cytotoxic Activity. Letters in Drug Design and Discovery, 2 (3). pp. 189-192. 10.2174/1570180053765075.
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An expeditious four-step synthesis of the 1H-pyrrolo[2,3-f]quinoline-2- carboxamides (5a-h) is described. Readily available 6-quinolinecarboxaldehyde is converted to the parent acid (6) by nucleophilic attack of the azido-ester (9) and intramolecular cyclization of (10) followed by hydrolysis of the methyl ester (11). The cytotoxicity of the target molecules (5a-h) was evaluated in four tumour cell lines in vitro. One compound (5d) showed sufficient activity (IC50 = 10.2 μM) in the human non-small cell lung cell line NSCLC-N16-L16 to be worthy of further study.
|Uncontrolled Keywords:||Cytotoxicity; Pyrrolo[2,3-f]quinolines; Synthesis|
|Departments, units and centres:||Department of Pharmaceutical and Biological Chemistry > Department of Pharmaceutical and Biological Chemistry|
|Journal or Publication Title:||Letters in Drug Design and Discovery|
|Deposited By:||Library Staff|
|Deposited On:||08 Mar 2012 10:48|
|Last Modified:||08 Mar 2012 10:48|
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