Letters in Drug Design & Discovery

Author(s): Andrew Tsotinis, Marilena Vlachou, Maria Gerasimopoulou, Aphrodite Eikosipentaki, Constantine Ioannidis, Anna Klouvidaki, Pandelis A. Afroudakis, Dimitri Moreau and Christos Roussakis

DOI: 10.2174/157018007779422488

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Symmetrical Derivatives of C2-Substituted Pyrrolo[2,3-f]quinolines:Synthesis, Cytotoxicity and Drug Delivery Studies

Page: [87 - 91] Pages: 5

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Abstract

The synthesis, pharmacological properties and delivery characteristics in simulated aqueous gastric fluid of a series of symmetrical nitrogenated C2-substituted pyrrolo[2,3-f]quinolines are described. The cytotoxicity of the target molecules (5a-h) was evaluated in the human non-small lung cancer cell line NSCLCN16- L16 in vitro. One compound (5e) showed sufficient activity (IC50 = 26.4 μM) and satisfactory release characteristics from solid pharmaceutical formulations.

Keywords: Symmetrical pyrrolo[2,3-f]quinolines, Synthesis, Cytotoxicity, Drug delivery