Xiaojing Li, Lei Li, Qin Zhou
Dec 15, 2014
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Influential Citations
7
Citations
Quality indicators
Journal
Bioorganic & medicinal chemistry letters
Abstract
A novel series of elemonic acid derivatives were synthesized and evaluated for their inhibitory activity on Pin1. Five compounds displayed significantly improved ability to inhibit Pin1 activity at micromolar levels. Compound 10 with 2-carboxylmethylene was the most active one with an IC50 value of 0.57 μM. The docking models of Pin1 support that introduction of an acidic group to elemonic acid enhance the Pin1 inhibitory activity.