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Rational design, synthesis and structure-activity relationships of antitumor (E)-2-benzylidene-1-tetralones and
1The Sam and Rose Stein Institute for Research on Aging and Department of Medicine, University of California San Diego, La Jolla 92093-0663, USA. hshih@ucsd.edu
Bioorganic & Medicinal Chemistry Letters
|April 1, 2000
Abstract:
Novel substituted 6,7-dimethoxy-1-tetralones and 5,6-dimethoxy-1-indanones have been synthesized and evaluated for their cytotoxicity. Compounds with 3'-lipophilic, 3',5'-dilipophilic, or 3',5'-dilipophilic-4'-hydrophilic substituents on (E)-2-benzylidene moiety showed highly cytotoxic effects. The unique structure of 42 possibly matches the pharmacophore features for these cytotoxic compounds.