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
  • 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. [email protected]
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.