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  • Title: Synthesis and biological activity of alpha-bromoacryloyl lexitropsin conjugates.
    Author: Romagnoli R, Baraldi PG, Iaconinoto MA, Carrion MD, Tabrizi MA, Gambari R, Borgatti M, Heilmann J.
    Journal: Eur J Med Chem; 2005 Nov; 40(11):1123-8. PubMed ID: 16006014.
    Abstract:
    The design, synthesis and biological evaluation of lexitropsins bearing mixed heterocyclic and benzoheterocyclic moieties and tethered to an alpha-bromo acrylic moiety acting as alkylating moiety are reported, and structure-activity relationships determined. With respect to antiproliferative activity against L1210 and K562 cells, compounds 7 and 10 showed the greatest potency, while compounds 4 and 5 exhibit the lowest activity. Among the synthesized compounds 4-12, the derivative 10 was found to be the most potent member of this class and it is 70-fold more active than the bis-pyrrole counterpart 3 against L1210 cell line. In addition, the cytotoxicity of derivatives 5-12 against KB cells and the influence of different glutathione (GSH) concentrations on the cytotoxic effects was also investigated.
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