1. Academic Validation
  2. Synthesis, antitumor evaluation, and apoptosis-inducing activity of hydroxylated (E)-stilbenes

Synthesis, antitumor evaluation, and apoptosis-inducing activity of hydroxylated (E)-stilbenes

  • J Med Chem. 2005 Feb 24;48(4):1292-5. doi: 10.1021/jm049238e.
Cedric J Lion 1 Charles S Matthews Malcolm F G Stevens Andrew D Westwell
Affiliations

Affiliation

  • 1 Cancer Research U.K. Experimental Cancer Chemotherapy Research Group, Centre for Biomolecular Sciences, School of Pharmacy, University of Nottingham, UK.
Abstract

The parallel solution-phase synthesis of a series of 30 monohydroxylated (E)-stilbene analogues is described. In vitro screening revealed low micromolar activity (GI(50)) against the MDA MB 468 breast Cancer cell line. Activity in MDA MB 468 cells correlated with the ability to induce Apoptosis following drug treatment by the most potent agents in the series, e.g., 5dy and 5jy, an observation further reinforced by AnnexinV-FITC analysis and fluorescence microscopy.

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