TY - JOUR TI - A facile synthesis of C2-substituted pyrrolo[2,3-f]quinolines with cytotoxic activity AU - Tsotinis, A. AU - Vlachou, M. AU - Zouroudis, S. AU - Jeney, A. AU - Timár, F. AU - Thurston, D.E. AU - Roussakis, C. JO - Letters in Drug Design and Discovery PY - 2005 VL - 2 TODO - 3 SP - 189-192 PB - SN - null TODO - 10.2174/1570180053765075 TODO - 1h pyrrolo[2,3 f]quinoline 2 carboxamide derivative; 6 quinolinecarboxaldehyde; pyrrolo[2,3 f]quinoline derivative; quinoline derivative; unclassified drug, article; cyclization; cytotoxicity; drug hydrolysis; drug structure; drug synthesis; priority journal; tumor cell line TODO - 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. © 2005 Bentham Science Publishers Ltd. ER -