2. Academic Validation
  3. Rational design, synthesis and structure-activity relationships of antitumor (E)-2-benzylidene-1-tetralones and (E)-2-benzylidene-1-indanones

Rational design, synthesis and structure-activity relationships of antitumor (E)-2-benzylidene-1-tetralones and (E)-2-benzylidene-1-indanones

  • Bioorg Med Chem Lett. 2000 Mar 6;10(5):487-90. doi: 10.1016/s0960-894x(00)00032-9.
H Shih 1,  L Deng,  C J Carrera,  S Adachi,  H B Cottam,  D A Carson
Affiliations

Affiliation

  • 1 The 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
PMID: 10743954 DOI: 10.1016/s0960-894x(00)00032-9
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.

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