Synthesis and glucose-stimulate insulin secretion (GSIS) evaluation of vindoline derivatives

Bioorganic & Medicinal Chemistry Letters
2017.0

Abstract

It is demonstrated that natural product vindoline can enhance the glucose-stimulated insulin secretion (GSIS) in MIN6 cells with the EC50 value of 50.2μM. In order to improve the activities, a series of vindoline derivatives are synthesized and evaluated in MIN6 cells. Compounds 4, 8, 17 and 24 show about 4.5 times more effective stimulation insulin secretion ability (EC50: 10.4, 14.2, 11.0 and 12.7μM, respectively) than vindoline.

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