Next Generation Thiazolyl Ketone Inhibitors of Cytosolic Phospholipase A2 α: from Synthesis to Chemotherapeutic Mechanism of Action
Berit Johansen,
Felicity Ashcroft,
Asimina Bourmpoula
et al.
Abstract:Eicosanoids regulate the pathologies of inflammation and carcinogenesis and limiting their production by inhibiting group IVA cytosolic phospholipase A2 (cPLA2α) is a potential approach to cancer treatment. Here we report the synthesis of a new generation of thiazolyl ketone inhibitors of cPLA2α starting from compound GK470 (AVX235), and the discovery of a more potent and selective lead, GK420 (AVX420), with significant chemotherapeutic properties. A cancer cell line screen revealed the selective growth i… Show more
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