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

Synthesis and activity of novel indirubin derivatives

Six novel indirubin Derivatives was designed, synthesized and characterized. Their anti?enzyme and anti?tumor activity were evaluated against IDO1 enzyme and K562 tumor cells. Some of the compounds showed moderate to high activity and the preliminary structure activity relationship was discussed in this paper.A series of indirubin derivatives hydrochloride were obtained using a convenient and mild method from indirubin. The newly synthesized compounds and their derivatives were characterized by 1H NMR, 13C NMR and MS. Furthermore, we tested their IDO1 enzyme inhibitory activity and anti?proliferative activities in K562 tumor cells. The experimental results revealed that some of the compounds showed potential antienzyme and antitumor activity. Among of them, compound 4b exhibited certain inhibitory activity on IDO1 (IC50: 29.52 ?mol/L), and compound 4a displayed activity similar to indirubin in K562 tumor cells (IC50: 24.96 ?mol/L). This type of indirubin derivative is expected to have the potential to act as an immunologically?active antitumor drug, indicating that further research will be worthwhile.

» Author: Bin Sun, Jiahao Wang, Luohua Liu, Longfei Mao, Lizeng Peng, Yuwei Wang

» Reference: doi:10.1111/cbdd.13792

» Publication Date: 10/09/2020

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