6406-74-2Relevant articles and documents
Semicarbazone derivative serving as caspase-3 activator and application thereof
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, (2019/02/10)
The invention provides semicarbazone derivative serving as a caspase-3 activator and application thereof. A structural general formula of the semicarbazone derivative or pharmaceutically acceptable salts of the semicarbazone derivative is shown as a formula I shown in the description. The semicarbazone derivative disclosed by the invention can be applied to preparing of medicine for treating or preventing cancer diseases and other hyperplastic diseases; thus, treating or preventing the cancer diseases and other hyperplastic diseases, and the semicarbazone derivative has an excellent application prospect in the aspect of developing antineoplastic medicine.
Semicarbazone derivatives bearing phenyl moiety: Synthesis, anticancer activity, cell cycle, apoptosis-inducing and metabolic stability study
Ma, Junjie,Ni, Xin,Gao, Yali,Huang, Kun,Wang, Yu,Liu, Jiaan,Gong, Guowei
, p. 351 - 360 (2019/05/07)
A series of semicarbazone derivatives bearing phenyl moiety were synthesized and evaluated for the vitro anticancer activities in four human cancer cell lines (human colon cancer (HT29), human neuroblastoma (SK-N-SH), human breast cancer (MDA-MB-231), and human gastric cancer (MKN45)). Biological evaluation led to the identification of 11q and 11s, which showed excellent anticancer activities against tested cancer cell lines with IC50 values ranging from 0.32 to 1.57μM, respectively, while exhibiting weak cytotoxicity on the normal cells (human umbilical vein endothelial cell (HUVEC)). Flow cytometric assay for cell cycle and apoptosis revealed that 11q and 11s caused an arrest in the Sub-G1 cell cycle and inhibited proliferation of cancer cells by inducing apoptosis in a dose-dependent manner. Further enzymatic assay suggested that 11q and 11s could significantly activated procaspase-3 to caspase-3. Metabolic stability study indicated that 11q and 11s showed moderate stability in vitro in human and rat liver microsomes. In view of promising pharmacological activities of 11q and 11s, which had emerged as the valuable lead for further development in the treatment for cancer.
amino animal pen amine compound can be for amplifying the synthetic method (by machine translation)
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, (2016/10/09)
The present invention provides medical benzylamine compound containing amino novel process for the preparation of intermediates for synthesizing process. Use of relatively cheap and easy to get raw material, by a selective condensation and the reduction reaction, to obtain the relatively high yield intermediate. To the raw materials of this method, line good atom economy, simple reaction, is easy to control, after treatment is simple, high yield, and is easy to enlarge the production, less waste residues, the present invention can effectively and the production of low-cost synthetic intermediate. (by machine translation)