Letters in Drug Design & Discovery

G. Perry
University of Texas
San Antonio, TX
Email: lddd@benthamscience.org


4-Hydroxy-3-methoxyphenyl Substituted 3-methyl-tetrahydroquinoline Derivatives Obtained Through Imino Diels-Alder Reactions as Potential Antitumoral Agents

Author(s): Vladimir V. Kouznetsov, Diego R. Merchan Arenas, Francisco Arvelo, Josue S. Bello Forero, Felipe Sojo, Arturo Munoz.


Two series of 17 tetrahydroquinoline compounds (2,4-DAr-THQs and DSQs), in which the 4-methoxy-3- hydroxyphenyl (isovanillin) structural unit is incorporated, were tested for their potential human tumor cell growth inhibitory effect on MCF-7, SKBR-3, PC3, HeLa and for non-tumor cells (primary culture of human dermis fibroblast – control cells) for the first time. The THQ 8 is an interesting model for antitumoral drugs, displaying cytotoxic activity against MCF7, SKBR3 or PC3 (IC50 7.99 - 16.14 μM) with the selectivity index 3.4 for MCF7.

Keywords: Functionalized tetrahydroquinolines, Isoeugenol, Antitumoral agents, Lewis acid-catalyzed imino Diels-Alder reactions, Tetrahydroquinoline compounds, Antimalarial, Antioxidant, Antimycobacterial, Polyfunctionalized quinoline, Anticancer agents, Hemi-synthetic, Synthetiq agents, Imino Diels Alder cycloaddition, Ketimine precursors, HeLa (cervical epithelial carcinoma), Adriamycin, Eugenol, Quinoline derivatives, Cytotoxic activities, Tumor cancer cells, Isatin, Anilines, Reference selectivity index

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Article Details

Year: 2010
Page: [632 - 639]
Pages: 8
DOI: 10.2174/157018010792929577
Price: $58