In this section, you can access to the latest technical information related to the FUTURE project topic.

Discovery of 3,3-di(indolyl)indolin-2-one as a novel scaffold for ?-glucosidase inhibitors: In silico studies and SAR predictions

3,3-Di(indolyl)indolin-2-ones 4a-4n were synthesized and evaluated for their in vitro ?-glucosidase inhibitory activity. These newly synthesized compounds showed moderate to potent ?-glucosidase inhibitory activity with IC50 range from 5.98±0.11 to 145.95±0.46?M, when compared to the standard drug acarbose. Among this series of 3,3-di(indolyl)indolin-2-ones, compound 4j (5.98±0.11?M) having a 2-fluorobenzyl group on the indole ring was found to be the most active compound. Molecular docking studies showed that compound 4j have high binding affinities with the active site of ?-glucosidase enzyme through hydrogen bonds, arene-cation, ?-? stacking and hydrophobic interactions. This study showed these 3,3-di(indolyl)indolin-2-ones as a new class of ?-glucosidase inhibitors.

» Author: Guangcheng Wang, Jing Wang, Zhenzhen Xie, Ming Chen, Luyao Li, Yaping Peng, Shan Chen, Wenbiao Li, Bin Deng

» Reference: Bioorganic Chemistry, Volume 72

» Publication Date: 01/06/2017

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