20776-45-8Relevant articles and documents
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Hamlin,Fischer
, p. 5007 (1951)
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Anti-tumor compounds
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Paragraph 0056; 0057; 0058; 0059; 0060, (2019/01/08)
The invention discloses anti-tumor compounds. The compounds target a Neddylation pathway. The compounds have a structural formula represented in a general formula I or a general formula II or a general formula III or a general formula IV or a general formula V or a general formula VI. The compounds have good anti-tumor activity, and multiple compounds are close to a positive control drug MLN4924,and can be used as good anti-tumor compounds. A combined therapy is provided through combined adoption of the compounds and compositions with other drugs, and a part of the same compositions can be formed by the drugs, or the drugs can be administered as separate components at the same time or at different time.
Synthesis and biological evaluation of novel tetrahydro-β-carboline derivatives as antitumor growth and metastasis agents through inhibiting the transforming growth factor-β signaling pathway
Zheng, Cong,Fang, Yuanzhang,Tong, Weiguang,Li, Guoliang,Wu, Haigang,Zhou, Wenbo,Lin, Qingxiang,Yang, Feifei,Yang, Zhengfeng,Wang, Peng,Peng, Yangrui,Pang, Xiufeng,Yi, Zhengfang,Luo, Jian,Liu, Mingyao,Chen, Yihua
, p. 600 - 612 (2014/03/21)
The transforming growth factor beta (TGFβ) signaling cascade is considered as one of the pivotal oncogenic pathways in most advanced cancers. Inhibition of the TGFβ signaling pathway by specific antagonists, neutralizing antibodies, or small molecules is considered as an effective strategy for the treatment of tumor growth and metastasis. Here we demonstrated the identification of a series of tetrahydro-β-carboline derivatives from virtual screening which potentially inhibit the TGFβ signaling pathway. Optimization of the initial hit compound 2-benzoyl-1,3,4,9-tetrahydro-β- carboline (8a) through substitution at different positions to define the structure-activity relationship resulted in the discovery of potent inhibitors of the TGFβ signaling pathway. Among them, compound 8d, one of the tested compounds, not only showed potent inhibition of lung cancer cell proliferation and migration in vitro but also strongly suppressed growth of lung cancer and breast cancer in vivo.
