Li Xinglin, Wu Shanchao, Dong Guoqiang, Chen Shuqiang, Ma Zonglin, Liu Dan, Sheng Chunquan
Key Laboratory of Structure-Based Drugs Design & Discovery of Ministry of Education, Shenyang Pharmaceutical University, Shenyang, Liaoning 110016, People's Republic of China.
Department of Medicinal Chemistry, School of Pharmacy, Second Military Medical University, 325 Guohe Road, Shanghai 200433, People's Republic of China.
ACS Med Chem Lett. 2020 Feb 28;11(4):439-444. doi: 10.1021/acsmedchemlett.9b00513. eCollection 2020 Apr 9.
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 could be triggered by reactive oxygen species (ROS) in the HCT116 colon cancer cell line and showed excellent antitumor activity and . It induced apoptosis in HCT116 cancer cells in a dose-dependent manner and cell growth arrest at the G2 phase.
为了提高天然产物吴茱萸碱的抗肿瘤效力，通过引入硼酸和硼酸盐作为触发单元，设计了新型含硼吴茱萸碱衍生物。硼酸盐衍生物可被HCT116结肠癌细胞系中的活性氧（ROS）触发，并表现出优异的抗肿瘤活性。它以剂量依赖的方式诱导HCT116癌细胞凋亡，并使细胞生长停滞在G2期。
