Abstract
A series of formylchromone derivatives were synthesized as PTP1B inhibitors and some of them were potent against PTP1B with IC 50 values as low as 1.0 μM. They exhibited remarkable selectivity for PTP1B over other human PTPases. Kinetic studies revealed that formylchromone derivatives are irreversible and active site-directed inhibitors. Molecular modeling study identified the orientation of the inhibitor bound at the active site of PTP1B.
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