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Synthesis and activity of novel indirubin derivatives
Chemical Biology & Drug Design ( IF 3.2 ) Pub Date : 2020-09-10 , DOI: 10.1111/cbdd.13792 Bin Sun 1 , Jiahao Wang 2 , Luohua Liu 3 , Longfei Mao 2 , Lizeng Peng 2 , Yuwei Wang 4, 5
Chemical Biology & Drug Design ( IF 3.2 ) Pub Date : 2020-09-10 , DOI: 10.1111/cbdd.13792 Bin Sun 1 , Jiahao Wang 2 , Luohua Liu 3 , Longfei Mao 2 , Lizeng Peng 2 , Yuwei Wang 4, 5
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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 anti‐enzyme and anti‐tumor activity. Among of them, compound 4b exhibited certain inhibitory activity on IDO1 (IC50: 29.52 μmol/L), and compound 4a displayed activity similar to indirubin in K562 tumor cells (IC50: 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.
中文翻译：
新型靛玉红衍生物的合成与活性
使用简便、温和的方法从靛玉红中获得了一系列靛玉红衍生物盐酸盐。新合成的化合物及其衍生物通过1 H NMR、13 C NMR 和 MS进行表征。此外，我们测试了它们在 K562 肿瘤细胞中的 IDO1 酶抑制活性和抗增殖活性。实验结果表明，一些化合物显示出潜在的抗酶和抗肿瘤活性。其中，化合物4b对IDO1表现出一定的抑制活性(IC 50 : 29.52 μmol/L)，化合物4a在K562肿瘤细胞中表现出与靛玉红相似的活性(IC 50: 24.96 μmol/L)。这种类型的靛玉红衍生物有望成为一种具有免疫活性的抗肿瘤药物，这表明进一步的研究是值得的。
更新日期：2020-09-10
中文翻译：
新型靛玉红衍生物的合成与活性
使用简便、温和的方法从靛玉红中获得了一系列靛玉红衍生物盐酸盐。新合成的化合物及其衍生物通过1 H NMR、13 C NMR 和 MS进行表征。此外，我们测试了它们在 K562 肿瘤细胞中的 IDO1 酶抑制活性和抗增殖活性。实验结果表明，一些化合物显示出潜在的抗酶和抗肿瘤活性。其中，化合物4b对IDO1表现出一定的抑制活性(IC 50 : 29.52 μmol/L)，化合物4a在K562肿瘤细胞中表现出与靛玉红相似的活性(IC 50: 24.96 μmol/L)。这种类型的靛玉红衍生物有望成为一种具有免疫活性的抗肿瘤药物，这表明进一步的研究是值得的。
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