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  • Title: Design, synthesis and biological evaluation of novel stilbene-based antitumor agents.
    Author: Simoni D, Invidiata FP, Eleopra M, Marchetti P, Rondanin R, Baruchello R, Grisolia G, Tripathi A, Kellogg GE, Durrant D, Lee RM.
    Journal: Bioorg Med Chem; 2009 Jan 15; 17(2):512-22. PubMed ID: 19117761.
    Abstract:
    A series of novel stilbene derivatives has been synthesized and studied with the main goal to investigate SAR of the amino compound 1a, as well as to improve its water solubility, a potentially negative aspect of the molecule that could be a serious obstacle for a pre-clinical development. We have obtained derivatives with good cytotoxic activity, in particular, the derivatives 5c and 6b could represent two novel leads for further investigation. Compound 8b, a morpholino-carbamate derivative, prodrug of 1a, has a very good solubility in water, and is active in suppressing growth of tumor cells at a concentration of 5000 nM, which is a concentration 100 times higher than the parent stilbene 1a.
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