Cyclometalated rhodium complexes were synthesized and evaluated as JAK2 metal-based inhibitors. Complexes 1 and 2 inhibited JAK2 enzyme phosphorylation activity, reduced JAK2 autophosphorylation in cellulo and exhibited cytotoxicity towards HEL cancer cells. To our knowledge, these are the first two examples of metal-based inhibitors of JAK2.
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Leung et al. (2012) studied this question.
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