1236876-86-0Relevant articles and documents
Second generation β-elemene nitric oxide derivatives with reasonable linkers: potential hybrids against malignant brain glioma
Bai, Renren,Zhu, Junlong,Bai, Ziqiang,Mao, Qing,Zhang, Yingqian,Hui, Zi,Luo, Xinyu,Ye, Xiang-Yang,Xie, Tian
, p. 379 - 385 (2022/01/20)
Elemene is a second-line broad-spectrum anti-tumour drug that has been used in China for more than two decades. However, its main anti-tumour ingredient, β-elemene, has disadvantages, including excessive lipophilicity and relatively weak anti-tumour effic
Aurovertin B derivative as well as preparation method and application thereof
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, (2020/12/30)
The invention provides an aurovertin B derivative, a preparation method of the aurovertin B derivative, and an application of the aurovertin B derivative in the preparation of a medicine for treatingtriple negative breast cancer. The polarity of the aurov
Synthesis of cucurbitacin B derivatives as potential anti-hepatocellular carcinoma agents
Ge, Weizhi,Chen, Xinyi,Han, Fangzhi,Liu, Zhongquan,Wang, Tianpeng,Wang, Mengmeng,Chen, Yue,Ding, Yahui,Zhang, Quan
, (2019/01/04)
Cucurbitacin B shows potent activity against tumor cells, but its high toxicity limits its application in the clinic. A series of cucurbitacin B derivatives was synthesized and evaluated for their anti-hepatocellular carcinoma (HCC) activities against the HepG-2 cell line. These compounds were also tested for their toxicity against the L-O2 normal cell line. The compound with the most potential, 10b, exhibited potent activity against the HepG-2 cell line with an IC50 value of 0.63 μM. Moreover, compound 10b showed the highest TI value (4.71), which is a 14.7-fold improvement compared to its parent compound cucurbitacin B. A preliminary molecular mechanism study of 10b indicated that 10b could inhibit P-STAT3 to induce the activation of mitochondrial apoptotic pathways. An in vivo acute toxicity study indicated that the compound 10b has preferable safety and tolerability compared with cucurbitacin B. These findings indicate that compound 10b might be considered as a lead compound for exploring effective anti-HCC drugs.