Chemical Biology & Drug Design 2010-06-01

Synthesis, cytotoxicity and antileishmanial activity of some N-(2-(indol-3-yl)ethyl)-7-chloroquinolin-4-amines.

Elaine S Coimbra, Rafael Carvalhaes, Richard M Grazul, Patricia A Machado, Marcos V N De Souza, Adilson D Da Silva

Index: Chem. Biol. Drug Des. 75(6) , 628-31, (2010)

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Abstract

We report herein the condensation of 4,7-dichloroquinoline (1) with tryptamine (2) and D-tryptophan methyl ester (3). Hydrolysis of the methyl ester adduct (5) yielded the free acid (6). The compounds were evaluated in vitro for activity against four different species of Leishmania promastigote forms and for cytotoxic activity against Kb and Vero cells. Compound (5) showed good activity against the Leishmania species tested, while all three compounds displayed moderate activity in both Kb and Vero cells.