Inhibition of group IVA cytosolic phospholipase A2 (cPLA2α) is a potential approach for cancer treatment. Here, the authors report 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.
- Felicity J. Ashcroft
- Asimina Bourboula
- Berit Johansen