95041-90-0Relevant articles and documents
Dichloroacetic acid coupled diphenylethane compound as well as preparation method and application thereof
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, (2022/03/31)
The invention belongs to the technical field of medicine synthesis, and particularly relates to a dichloroacetic acid coupled diphenylethane compound as well as a preparation method and application thereof. The structure of the dichloroacetic acid coupled diphenylethane compound is shown as a general formula (I), R1, R2 and R3 are respectively selected from but not limited to any one of-OH,-OMe and H, R4 is selected from but not limited to any one of-OMe and-OEt, R5 and R6 are selected from chlorine atoms or fluorine atoms, m is 0 or 1, and n is a positive integer selected from 1-8 or 11-12. The dichloroacetic acid coupled diphenylethane compound disclosed by the invention is stable in structure, low in toxicity, simple and convenient in preparation process and high in yield, does not need to be stored in a dark place, has obvious anti-tumor activity on various tumor cells cultured in vitro, and is obvious in in-vivo anti-tumor effect. The general formula (I) is shown in the specification.
5-FLUOROURACIL DERIVATIVES, PREPARATION METHODS AND USES THEREOF
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, (2021/07/30)
Disclosed is a 5-fluorouracil derivative having the molecular structure shown in general formula VI, in which Ra and Rb groups are an alkoxy group or a fluorine-substituted alkoxy group having 1, 2, 3, or 4 carbon atoms, and are mono-, bis-, tri-, tetra- or penta-substituted on a phenyl group; a linking group L1 is an alkyl or alkenyl group having 1, 2, 3, or 4 carbon atoms, a linking group L2 is oxygen, or an alkyl or alkoxy group having 1, 2, 3, or 4 carbon atoms, or an amino acid, or an alkyl group having 1, 2, 3, or 4 carbon atoms containing an amino moiety, or a furyl group, and an X group is O or —NH—. Further disclosed is a method for preparing such a derivative and a use of the same in the treatment of cancer, tumor diseases, and diseases caused by abnormal neovascularization in a human or non-human mammal, and a medicament or a composition containing the 5-fluorouracil derivative.
Erianin, a novel dibenzyl compound in Dendrobium extract, inhibits bladder cancer cell growth via the mitochondrial apoptosis and JNK pathways
Zhu, Qiyu,Sheng, Yuwen,Li, Wenhua,Wang, Jing,Ma, Yulin,Du, Baowen,Tang, Yaxiong
, p. 41 - 54 (2019/04/26)
Erianin, a component extracted from the traditional Chinese herbal medicine Dendrobium, has shown significant anti-tumour activity in various cancers but not in bladder cancer. In this study, we assessed the effects of Erianin on bladder cancer growth and elucidated the related mechanisms. First, Erianin was synthesized with high yields, and markedly suppressed EJ and T24 cell proliferation. It induced G2/M-phase arrest in vitro. Furthermore, Erianin triggered apoptosis via caspase cascades activation and the mitochondrial-mediated apoptotic pathway. Bim up-regulation and Bcl-2 down-regulation as the symbol of apoptosis which were found to play the dominant role in the effects of Erianin. We further showed that JNK pathway activation is necessary for the Erianin-mediated anti-proliferation and apoptotic response. Finally, Erianin exhibited anti-tumour activity and induced apoptosis in tumour tissue in vivo. Collectively, these results suggest that Erianin induced cell cycle G2/M-phase arrest and apoptosis via the JNK signalling pathway in bladder cancer, indicating the potential usefulness of Erianin for the therapy of bladder cancer.