95-84-1Relevant academic research and scientific papers
Design, synthesis and biological evaluation of benz-fused five-membered heterocyclic compounds as tubulin polymerization inhibitors with anticancer activities
Komuraiah, Buduma,Ren, Yichang,Xue, Mingming,Cheng, Binbin,Liu, Jin,Liu, Yao,Chen, Jianjun
, p. 1109 - 1116 (2021/03/16)
A series of benz-fused five-membered heterocyclic compounds were designed and synthesized as novel tubulin inhibitors targeting the colchicine binding site. Among them, compound 4d displayed the highest antiproliferative activity against four cancer cell lines with an IC50 value of 4.9?μM in B16-F10 cells. Compound 4d effectively inhibited tubulin polymerization in vitro (IC50 of 13.1?μM). Further, 4d induced cell cycle arrest in G2/M phase. Finally, 4d inhibited the migration of cancer cells in a dose-dependent manner. In summary, these results suggest that compound 4d represents a new class of tubulin inhibitors deserving further investigation.
HMOX1 inducers
-
Page/Page column 88, (2020/09/18)
The present invention is related to compounds of structure (I) as heme oxygenase 1 (HMOX 1) inducers. The present invention is also related a method of controlling the activity or the amount, or both the activity and the amount, of heme-oxygenase 1 in a mammalian subject. The definitions of the variables are provided herein.
Record-high catalytic hydrogenated activity in nitroarenes reduction derived from in-situ nascent active metals enabled by constructing bimetallic phosphate
Yang, Fu,Wang, Jin,Gao, Shuying,Zhou, Shijian,Kong, Yan
, (2020/03/10)
Herein, we report an excellent in-situ exsolution triggered hydrogenated catalyst F-Ni/Cu-P-RT started from bimetallic phosphate Ni/Cu-P-RT, affording an ultrafast catalytic hydrogenated rate (20 s even 5 s) in nitrophenol reduction. In the first catalytic cycle, we proved the enhanced catalytic reduction activity of bimetallic Ni/Cu-P-RT within 50 s compared to monometallic counterparts. The kinetics results revealed Ni/Cu-P-RT affords the reaction rate K of 2.85/4.23/6.6 min?1 at 20, 30, and 40 °C with the activation energy 32 kJ/mol. Impressively, the involved reaction induction period is visibly observed and interpreted by reconstruction and evolution of active metal during the reaction, but was eliminated through integrating two metal Cu-Ni by regulation of electronic band energy of phosphate from 4.1–3.5 eV. The nascent Cu and Ni nanoparticles as reaction-preferred active species were in-situ exsolved partially after adding NaBH4, triggering the resulted higher active and stable F-Ni/Cu-P-RT(20 s, 14.1 min?1) in later multiple cycles.
Hydrogenation of Substituted Benzenes Containing Nitro and Azo Groups over Skeletal Nickel in Aqueous Solutions of 2-Propanol
An’, Khoang,Belova, A. V.,Lefedova, O. V.,Nemtseva, M. P.
, p. 720 - 724 (2020/04/24)
Abstract: An analysis is made of the kinetic characteristics of the hydrogenation of 4-nitro- and 2-nitro-2'-hydroxy-5'-methylazobenzenes, 4-nitroaniline and 4-aminoazobenzene over skeletal nickel in neutral azeotropic 2-propanol–water mixture and in the same solvent in the presence of acetic acid or sodium hydroxide. It is found that the selectivity of the hydrogenation of these isomers to the intermediate products depends on the composition and nature of the solvent, and is determined by the rate of reactive group conversion. Compared to the process in the presence of sodium hydroxide, which suppresses the route leading to the predominant hydrogenation of the nitro group, the contribution from the transformation of azo group is considerably greater in the hydrogenation of 4-nitro-2'-hydroxy-5'-methylazobenzene in the presence of acetic acid. Adding a base to the solvent during the hydrogenation of 2-nitro-2'-hydroxy-5'-methylazobenzene accelerates the rate of nitro group conversion and the intramolecular cyclization of the intermediate compound, increasing the selectivity towards the products containing the benzotriazole cycle (particularly 2-(2-hydroxy-5-methylphenyl)benzotriazole-N-oxide). The almost linear correlation between the selectivity of the catalytic hydrogenation of isomers of nitro-2'-hydroxy-5'-methylazobenzene and the kinetic characteristics of the hydrogenation of nitro and azo groups in compounds containing a single reactive substituent at different values of medium’s pH is estimated.
An Azo Coupling Strategy for Protein 3-Nitrotyrosine Derivatization
Liu, Yuxin,Zhou, Pengcheng,Da, Honghong,Jia, Huiyi,Bai, Feifei,Hu, Guodong,Zhang, Baoxin,Fang, Jianguo
supporting information, p. 11228 - 11232 (2019/08/07)
Herein, a strategy for the selective derivatization of 3-nitrotyrosine-containing proteins using the classic azo coupling reaction as the key step is described. This novel approach featured multiple advantages and was successfully applied to detect picomole levels of protein tyrosine nitration in biological samples.
Benzoxazole derivatives, method for preparing the same and pharmaceutical composition comprising the same
-
Paragraph 0194-0196, (2019/06/28)
The present invention refers to benzoxazole derivatives, stereoisomers, about number cosmetically acceptable salt, solvate or hydrate number [...] substrate. (by machine translation)
The Continuous Synthesis of 2-(2'-Hydroxy-5'-Methylphenyl)Benzotriazole over Cu/γ-Al2O3
Yan,Si,Tao,Liu,Wang,Li
, p. 635 - 641 (2019/10/19)
Abstract: The samples of 20% Cu/γ-Al2O3, 20% Co/γ-Al2O3 and 20% Ni/γ-Al2O3 were prepared as hydrogenation catalysts for continuous synthesis of 2-(2'-hydroxy-5'-methylphenyl)benzotriazole. The best yield (86.62%) was afforded by the 20% Cu/γ-Al2O3 catalyst. The characterizations results obtained for the 20% Cu/γ-Al2O3 sample confirmed that Cu particles are evenly distributed over the surface of γ-Al2O3. A reduction of acid sites in the catalyst favored the selectivity to 2-(2'-hydroxy-5'-methylphenyl)benzotriazole. Furthermore, the effect of Cu content, reaction temperature, hydrogen pressure and liquid hourly space velocity was studied. Finally, 2-(2'-hydroxy-5'-methylphenyl)benzotriazole in 86.62% yield was attained under the optimized conditions.
A 2 - [d] oxazole chlorobenzene and -5 - preparation of formic acid method (by machine translation)
-
Paragraph 0020; 0021; 0022, (2017/12/27)
The invention discloses a 2 - chlorobenzene and [d] oxazole - 5 - carboxylic acid, in order to 2 - nitro - 4 - methyl phenol as the starting material, passes through the reduction, ring, chlorinated, oxidation to obtain the target product, the compound is an important medical intermediates. (by machine translation)
Preparation method for methylthio-substituted benzo[d]oxazole derivative
-
Paragraph 0019; 0020, (2017/08/31)
The invention discloses a preparation method for a methylthio-substituted benzo[d]oxazole derivative, i.e., 5-methyl-2-(methylthio)benzo[d]oxazole. According to the invention, 2-nitro-4-methylphenol is used as a starting raw material and undergoes reduction, ring closure and methylation so as to obtain the methylthio-substituted benzo[d]oxazole derivative. The prepared derivative is an important medical intermediate.
Catalytic hydrogenation of 2-nitro-2′-hydroxy-5′-methylazobenzene over solid base-hydrogenation bifunctional catalysts: Effect of alkali metals on Pd/γ-Al2O3
Si, Leilei,Wang, Bowei,Chen, Shipeng,Hou, Jingru,Yan, Xilong,Li, Yang,Chen, Ligong
, p. 35 - 38 (2016/11/25)
Alkali metals doped Pd solid base-hydrogenation bifunctional catalysts were prepared, characterized, and employed in the hydrogenation of 2-nitro-2′-hydroxy-5′-methylazobenzene. The results indicated that the basicity of catalyst endowed by the alkali met
