0000000000750250
AUTHOR
Irina Chuckowree
showing 2 related works from this author
Synthesis of hybrid anticancer agents based on kinase and histone deacetylase inhibitors
2014
Fragments based on the VEGFR2i Semaxanib (SU5416, (vascular endothelial growth factor receptor-2\ud inhibitor) and the HDACi (histone deacetylase inhibitor) SAHA (suberanilohydroxamic acid) have been\ud merged to form a range of low molecular weight dual action hybrids. Vindication of this approach is\ud provided by SAR, docking studies, in vitro cancer cell line and biochemical enzyme inhibition data as well\ud as in vivo Xenopus data for the lead molecule (Z)-N1-(3-((1H-pyrrol-2-yl)methylene)-2-oxoindolin-5-yl)-\ud N8-hydroxyoctanediamide 6.
Cytotoxicity of the Urokinase-Plasminogen Activator Inhibitor Carbamimidothioic Acid (4-Boronophenyl) Methyl Ester Hydrobromide (BC-11) on Triple-Neg…
2015
BC-11 is an easily synthesized simple thiouronium-substituted phenylboronic acid, which has been shown to be cytotoxic on triple negative MDA-MB231 breast cancer cells by inducing a perturbation of cell cycle when administered at a concentration equal to its ED50 at 72 h (117 μM). Exposure of cells to BC-11, either pre-absorbed with a soluble preparation of the N-terminal fragment of urokinase-plasminogen activator (uPa), or in co-treatment with two different EGFR inhibitors, indicated that: (i) BC-11 acts via binding to the N-terminus of the enzyme where uPa- and EGF receptor-recognizing sites are present, thereby abrogating the growth-sustaining effect resulting from receptor binding