Τίτλος:
A facile synthesis of C2-substituted pyrrolo[2,3-f]quinolines with cytotoxic activity
Γλώσσες Τεκμηρίου:
Αγγλικά
Περίληψη:
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.
Συγγραφείς:
Tsotinis, A.
Vlachou, M.
Zouroudis, S.
Jeney, A.
Timár, F.
Thurston, D.E.
Roussakis, C.
Περιοδικό:
Letters in Drug Design and Discovery
Λέξεις-κλειδιά:
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
DOI:
10.2174/1570180053765075
