Natural Product Evodiamine with Borate Trigger Unit: Discovery of Potent Antitumor Agents against Colon Cancer

ACS Med Chem Lett. 2020 Feb 28;11(4):439-444. doi: 10.1021/acsmedchemlett.9b00513.

Xinglin Li ¹, Shanchao Wu ², Guoqiang Dong ², Shuqiang Chen ², Zonglin Ma ¹, Dan Liu ¹, Chunquan Sheng ²

Affiliations

1 Key Laboratory of Structure-Based Drugs Design & Discovery of Ministry of Education, Shenyang Pharmaceutical University, Shenyang, Liaoning 110016, People's Republic of China.
2 Department of Medicinal Chemistry, School of Pharmacy, Second Military Medical University, 325 Guohe Road, Shanghai 200433, People's Republic of China.

PMID: 32292547 DOI: 10.1021/acsmedchemlett.9b00513

Abstract

In order to improve the antitumor potency of the natural product evodiamine, novel boron-containing evodiamine derivatives were designed by incorporating boronic acid and boronate as trigger units. Boronate derivative 13a could be triggered by Reactive Oxygen Species (ROS) in the HCT116 colon Cancer cell line and showed excellent antitumor activity in vitro and in vivo. It induced Apoptosis in HCT116 Cancer cells in a dose-dependent manner and cell growth arrest at the G2 phase.

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