Large-scale semi-synthesis of indirubin from Strobilanthes cusia leaf extract and novel indirubin derivatives active against HT29 colon cancer cells

Large-scale semi-synthesis of indirubin from Strobilanthes cusia leaf extract and novel indirubin derivatives active against HT29 colon cancer cells Научная публикация

Журнал

Journal of Tropical Science and Engineering
ISSN: 3093-3633

Вых. Данные

Год: 2026, Том: 1, Номер: 2, Страницы: 60-72 Страниц : 13 DOI: 10.58334/jtse.vol.001.849

Авторы

Nguyen Trong Dan ¹ , Pham Duy Nam ¹ , Vu Dinh Duy ¹ , Vu Duy Nhan ¹ , Vo Thi Hoai Thu ¹ , Hoang Quang Cuong ¹ , Hoang Duc Quang ¹ , Fomenkov Dimitri Igorevich ² , Ilovaisky Alexey Igorevich ² , Yaremenko Ivan Andreevich ² , Terent'ev Alexander Olegovich ² , Bui Thi Thu Trang ³

Организации

1	Joint Vietnam-Russia Tropical Science and Technology Research Center, Hanoi, Vietnam
2	N. D. Zelinsky Institute of Organic Chemistry, Russian Academy of Sciences, Moscow, Russian Federation
3	Vietnam Faculty of Chemical Technology, Hanoi University of Industry (HaUI), Hanoi, Vietnam

In this study, indirubin with a purity exceeding 97% was synthesized from Strobilanthes cusia leaf extract and isatin. Subsequently, this was used as the starting material for the synthesis of eight new indirubin-3’-oxime derivatives. These compounds, bearing substituents containing a bromine atom (3b, 3c), an azide group (4a–c), or 2-amino-1,3,4-thiadiazole moiety (5a–c), were successfully synthesized in yields ranging from 75% to 88%. The chemical structures of all compounds were elucidated using modern spectroscopic techniques, including 1H and 13C NMR spectroscopy, High-Resolution Electrospray Ionization Mass Spectrometry (HR-MS (ESI)), and Infra Red (IR) spectroscopy. The cytotoxic activity of the synthesized compounds was evaluated against the HT29 human colon cancer cell line. Indirubin derivatives 5b and 5c exhibited potent cytotoxic activity, with IC50 values of 3.2 ± 0.1 µM and 6.2 ± 0.2 µM, respectively. Both compounds were more potent than the parent indirubin (1a) and the positive control, 5-fluorouracil. Overall, the synthesized indirubin derivatives represent a valuable synthetic platform for the further development of novel indirubin-based bioactive compounds in medicinal chemistry and anticancer drug discovery.

Nguyen T.D. , Pham D.N. , Vu D.D. , Vu D.N. , Vo T.H.T. , Hoang Q.C. , Hoang D.Q. , Fomenkov D.I. , Ilovaisky A.I. , Yaremenko I.A. , Terent'ev A.O. , Bui T.T.T.
Large-scale semi-synthesis of indirubin from Strobilanthes cusia leaf extract and novel indirubin derivatives active against HT29 colon cancer cells
Journal of Tropical Science and Engineering. 2026. V.1. N2. P.60-72. DOI: 10.58334/jtse.vol.001.849 OpenAlex

Поступила в редакцию:	9 февр. 2026 г.
Опубликована online:	16 июн. 2026 г.

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