6406-74-2Relevant academic research and scientific papers
Semicarbazone derivative serving as caspase-3 activator and application thereof
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Paragraph 0081; 0087-0089, (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.
Identification and biological evaluation of novel benzothiazole derivatives bearing a pyridine-semicarbazone moiety as apoptosis inducers via activation of procaspase-3 to caspase-3
Ma, Junjie,Ni, Xin,Gao, Yali,Huang, Kun,Liu, Jiaan,Wang, Yu,Chen, Roufen,Wang, Cuifang
, p. 465 - 477 (2019/03/28)
Three series of compounds were designed, synthesized and evaluated for their in vitro anticancer activity against a procaspase-3 over-expression cancer cell line (U937) and a procaspase-3 no-expression cancer cell line (MCF-7) to rule out off-target effects. Biological evaluation led to the identification of a series of benzothiazole derivatives bearing a pyridine-semicarbazone moiety, 8j and 8k, with promising anticancer activity and remarkable selectivity. Further mechanism studies revealed that compounds 8j and 8k could induce apoptosis of cancer cells by activating procaspase-3 to caspase-3, and compound 8k exhibited the strongest procaspase-3 activation activity. Structure-activity relationships (SARs) revealed that the presence of benzothiazole and an N,N,O-donor set is crucial for the anticancer activity and selectivity, and reducing the electron density of the N,N,O-donor set results in a dramatic decline in the anticancer activity and selectivity. Furthermore, toxicity evaluation (zebrafish) in vivo and metabolic stability studies (human, rat and mouse liver microsomes) were performed to provide reliable guidance for further PK/PD studies in vivo.
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.
COVALENT ORGANIC FRAMEWORK FOR ADSORBING SO2 GAS AND METHOD FOR PREPARING THE SAME
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Paragraph 0104-0109, (2018/09/02)
The present invention refers to SO2 Gas adsorption number is suitable as a covalent organic frameworks structure (Covalent Organic Framework, COF) and manufacturing method relates to search, imide structure has backbone of the present invention covalent organic frameworks, SO2 6 Frame of network architecture having a polar group having reactive porous are disclosed. (by machine translation)
amino animal pen amine compound can be for amplifying the synthetic method (by machine translation)
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Paragraph 0039; 0041; 0040, (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)
OMEGA-AMINOALKYLAMIDES OF (R)-2-ARYL-PROPIONIC ACIDS AS INHIBITORS OF THE CHEMOTAXIS OF POLYMORPHONUCLEATE AND MONONUCLEATE CELLS
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Paragraph 0095, (2016/08/23)
no abstract published
Design, synthesis and antiproliferative activity of novel benzothiazole derivatives conjugated with semicarbazone scaffold
Bao, Guanglong,Du, Baoquan,Ma, Yuxiu,Zhao, Meng,Gong, Ping,Zhai, Xin
, p. 489 - 498 (2016/07/19)
Two series of novel benzothiazole derivatives conjugated with semicarbazone scaffold were designed and synthesized through a structure-based molecular hybridization strategy. All the target compounds were evaluated for their cytotoxicity in vitro against three cancer cell lines (HT-29, MKN-45 and H460) by standard MTT assay. The pharmacological results indicated that seven compounds (17h-n) exhibited comparable or even better antiproliferative activity in comparison with reference drugs Sorafenib and PAC-1. Particularly, compound 17i displayed remarkable cytotoxicity against tested three cancer cell lines with IC50 values of 0.84, 0.06 and 0.52 μM, which were 4.3-, 36.6-, 4.2-folds more potent than Sorafenib and 1.2-, 13.7-, 6.9-times more active than PAC-1, respectively.
Hydrogenation of (N,N-disubstituted aminomethyl)nitrobenzenes to (N,N-disubstituted aminomethyl)anilines catalyzed by palladium-nickel bimetallic nanoparticles
Bao, Hailin,Wang, Dingsheng,Wang, Xinyan,Cheng, Chuanjie,Li, Yadong,Hu, Yuefei
, p. 47125 - 47130 (2015/06/16)
Since palladium-catalysts have strong abilities for both hydrogenation of nitro-group and hydrogenolysis of benzylamine, they have a much lower chemoselectivity for the hydrogenation of (N,N-disubstituted aminomethyl)nitrobenzenes. In this article, component stable Pd-Ni bimetallic nanoparticles were prepared by simply heating RANEY-Ni and Na2PdCl4 together in water. They demonstrated novel synergistic effects when they were used as a bimetallic catalyst, by which a highly efficient and chemoselective hydrogenation of (N,N-disubstituted aminomethyl)nitrobenzenes to (N,N-disubstituted aminomethyl)anilines was achieved.
TETRACYCLIC ANTHRAQUINONE DERIVATIVES
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Paragraph 0105, (2015/02/02)
Disclosed are a compound represented by formula (I) and a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, W, n are defined as in the present application.
Tetracyclic Anthraquinone Derivatives
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Paragraph 0223, (2015/06/24)
Disclosed are a compound represented by formula (I) and a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, W, n are defined as in the present application.
