10113-40-3Relevant academic research and scientific papers
Phosphotungstic acid supported on silica-coated CoFe2O4 nanoparticles: An efficient and magnetically-recoverable catalyst for N-formylation of amines under solvent-free conditions
Kooti,Nasiri
, p. 168 - 177 (2015)
Phosphotungstic acid (PTA) was rapidly and efficiently anchored on the surface of silica coated cobalt ferrite core to obtain a new three-component CoFe2O4@SiO2-PTA nanocomposite. The resultant composite was characterized by various techniques, including FT-IR, XRD, SEM, EDX, ICP-AES, and VSM. The as-synthesized nanocomposite was examined as catalyst for N-formylation of various amines under solvent-free conditions at room temperature. Due to the presence of magnetic core in this catalyst, it can be easily separated from the reaction media by applying an external magnetic field. The isolated catalyst can be reused for at least five successive times without significant leaching or loss of its high catalytic activity.
A capable cobalt nano-catalyst for the N-formylation of various amines and its biological activity studies
Habibi, Davood,Heydari, Somayyeh,Afsharfarnia, Mina
, (2017)
The Fe3O4 magnetic nanoparticles (Fe3O4 MNPs) were modified with 1,10-phenanthroline-5,6-diol and the relevant Co complex (Fe3O4@Phendiol@Co) synthesized as a nano-magnetic heterogeneous catalyst to be used for the N-formylation of various amines at room temperature under solvent-free conditions. Also, in order to find the better concept of the catalyst role, the N-formylation reaction was carried out by the use of ultrasound irradiation in the absence of the Co nano-catalyst and the results were compared. The catalyst characterized by different methods such as the elemental analysis (CHN), ICP, FT-IR, XRD, EDX, SEM, TEM, TG-DTA, VSM and XPS. In addition, the antioxidant and the antibacterial activities of the Fe3O4@Phendiol@Co nano-catalyst and its Phendiol ligand were in vitro screened by 2,2-diphenyl-1-picrylhydrazyl (DPPH) free radical scavenging and disc diffusion methods. Results showed that they possess strong antioxidant activity (IC50; 0.182?±?0.006?mg/ml) and good antibacterial potential in comparison to standards.
Design, synthesis and anticancer evaluation of 3-methyl-1H-indazole derivatives as novel selective bromodomain-containing protein 4 inhibitors
Dong, Ru,Zhang, Cheng,Wang, Chao,Zhou, Xin,Li, Wen,Zhang, Jin-Yang,Wang, Min,Xu, Yong,Sun, Li-Ping
, (2022/01/11)
Bromodomain-containing Protein 4 (BRD4), an ‘epigenetic reader’, regulates chromatin structure and gene expression via recognizing and binding acetylated lysine in histones. BRD4 has become a therapeutic target for cancers because it promotes the expression of the tumor genes, such as c-Myc, NF-κB, and Bcl-2. In this study, a new series of 3-methyl-1H-indazole derivatives were designed via virtual screening and structure-based optimization. All compounds were synthesized and evaluated for their inhibitory activities to BRD4-BD1 and their antiproliferative effects in cancer cell lines. Among them, several compounds (such as 9d, 9u and 9w) exhibited strong BRD4-BD1 affinities and inhibition activities, and potently suppressed MV4;11 cancer cell line proliferation. Among them, compound 9d showed excellent selectivity for BRD4 and effectively suppressed c-Myc, the downstream protein of BRD4. This study provided new lead compounds for further biological evaluation on BRD4.
Design, synthesis and biological evaluation of novel 4-(2-fluorophenoxy)quinoline derivatives as selective c-Met inhibitors
Wang, Xiaoqiang,Jiang, Nan,Zhao, Sijia,Xi, Shuancheng,Wang, Jiao,Jing, Tongfei,Zhang, Wenyu,Guo, Ming,Gong, Ping,Zhai, Xin
, p. 886 - 896 (2017/02/05)
Two novel series of 6,7-disubstituted-4-(2-fluorophenoxy)quinoline derivatives bearing 1H-imidazole-4-carboxamido or (E)-3-hydrosulfonylacrylamido motifs (16–31 and 32–42) were designed, synthesized and evaluated for their in vitro cytotoxic activity. Most of the compounds exhibited moderate to excellent potency against tested three cell lines, and fifteen compounds were further examined for their inhibitory activity against c-Met kinase. The most promising compound 16 (c-Met kinase [IC50]?=?1.1?nM) demonstrated high selectivity and remarkable cytotoxicity against HT-29, MKN-45 and A549 cells with IC50values of 0.08, 0.22 and 0.07?μM, which were 3.1-, 1.4- and 2.1-fold more active than Foretinib. The preliminary structure-activity relationships as well as molecular docking disclosed that 1H-imidazole-4-carboxamido as a linker was of great importance for the antitumor activity.
