Regio-selective synthesis and activity research on 7-icaritin norcantharidin conjugates

Abstract

Due to complexity of tumor diseases and resistance of targeted drug, targeted drug usually cannot meet the needs of cancer treatment. Therefore, the conjugate constructed by two anticancer agents maybe a better solution for the tumor diseases. As natural anticancer agents, icaritin and norcantharidin are selected for the construction of conjugate. In the condition of EDCI/DMAP, icaritin is reacted with norcantharidin esters to give the desired 7-esters selectively in a moderate yield. MTT method was used to test the cytotoxicity and intensity on Hep G2 and MCF-7 in vitro. Some of the compounds (4a, 4i and 4j) show a better inhibition against Hep G2 and MCF-7 cell lines in vitro, and are deserved to be a potential drug candidate to develop in vivo.

Keywords:

• Icaritin
• conjugate
• norcantharidin
• anti-cancer

Acknowledgements

I’d like to express my thanks to the financial support from Key Project of Guizhou Provincial Administration of Traditional Chinese Medicine (QZYY-2021-086), Science and Technology Department of Guizhou Province (QKHSY [2017]2844) and (QKHSY [2015]3030), Joint Funds of Zunyi City (CK-1187-041) and science and technology fund project of Guizhou provincial health commission (GZWKJ2022-220). I am also thankful for Dr. Jianyong zhang’s useful explanation on HPLC and HRMS spectra data.

Disclosure statement

No potential conflict of interest was reported by the authors.

Additional information

Funding

I’d like to express my thanks to the financial support from Key Project of Guizhou Provincial Administration of Traditional Chinese Medicine (QZYY-2021-086), Science and Technology Department of Guizhou Province (QKHSY [2017]2844) and (QKHSY [2015]3030), Joint Funds of Zunyi City (CK-1187-041) and science and technology fund project of Guizhou provincial health commission (GZWKJ2022-220). I am also thankful for Dr. Jianyong zhang’s useful explanation on HPLC and HRMS spectra data.