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Synthesis and activity of novel indirubin derivatives
Author(s) -
Sun Bin,
Wang Jiahao,
Liu Luohua,
Mao Longfei,
Peng Lizeng,
Wang Yuwei
Publication year - 2021
Publication title -
chemical biology and drug design
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.59
H-Index - 77
eISSN - 1747-0285
pISSN - 1747-0277
DOI - 10.1111/cbdd.13792
Subject(s) - indirubin , chemistry , stereochemistry , enzyme , inhibitory postsynaptic potential , derivative (finance) , k562 cells , tumor cells , combinatorial chemistry , biochemistry , in vitro , biology , medicine , cancer research , indigo , art , financial economics , economics , visual arts
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 1 H NMR, 13 C 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 anti‐enzyme and anti‐tumor activity. Among of them, compound 4b exhibited certain inhibitory activity on IDO1 (IC 50 : 29.52 μmol/L), and compound 4a displayed activity similar to indirubin in K562 tumor cells (IC 50 : 24.96 μmol/L). This type of indirubin derivative is expected to have the potential to act as an immunologically active anti‐tumor drug, indicating that further research will be worthwhile.