4385-62-0Relevant academic research and scientific papers
New cyclometalated iridium(III) dye chromophore complexes for p-type dye-sensitised solar cells
Sinopoli, Alessandro,Wood, Christopher J.,Gibson, Elizabeth A.,Elliott, Paul I.P.
, p. 269 - 277 (2017)
The synthesis of seven iridium complexes [Ir(C?N)2(N?N)][PF6] (AS9-15) designed as dyes for p-type DSSC is described. These complexes comprise a 4-(pyrid-2-yl)benzoic acid as the cyclometalating/anchoring ligand with different diimin
Photo-induced deep aerobic oxidation of alkyl aromatics
Wang, Chang-Cheng,Zhang, Guo-Xiang,Zuo, Zhi-Wei,Zeng, Rong,Zhai, Dan-Dan,Liu, Feng,Shi, Zhang-Jie
, p. 1487 - 1492 (2021/07/10)
Oxidation is a major chemical process to produce oxygenated chemicals in both nature and the chemical industry. Presently, the industrial manufacture of benzoic acids and benzene polycarboxylic acids (BPCAs) is mainly based on the deep oxidation of polyalkyl benzene, which is somewhat suffering from environmental and economical disadvantage due to the formation of ozone-depleting MeBr and corrosion hazards of production equipment. In this report, photo-induced deep aerobic oxidation of (poly)alkyl benzene to benzene (poly)carboxylic acids was developed. CeCl3 was proved to be an efficient HAT (hydrogen atom transfer) catalyst in the presence of alcohol as both hydrogen and electron shuttle. Dioxygen (O2) was found as a sole terminal oxidant. In most cases, pure products were easily isolated by simple filtration, implying large-scale implementation advantages. The reaction provides an ideal protocol to produce valuable fine chemicals from naturally abundant petroleum feedstocks. [Figure not available: see fulltext.].
Structure-based drug optimization and biological evaluation of tetrahydroquinolin derivatives as selective and potent CBP bromodomain inhibitors
Bi, Xiaoyang,Chen, Yu,Sun, Zhongya,Lu, Wenchao,Xu, Pan,Lu, Tian,Ding, Hong,Zhang, Naixia,Jiang, Hualiang,Chen, Kaixian,Zhou, Bing,Luo, Cheng
supporting information, (2020/09/16)
CBP bromodomain could recognize acetylated lysine and function as transcription coactivator to regulate transcription and downstream gene expression. Furthermore, CBP has been shown to be related to many human malignancies including acute myeloid leukemia. Herein, we identified DC-CPin734 as a potent CBP bromodomain inhibitor with a TR-FRET IC50 value of 19.5 ± 1.1 nM and over 400-fold of selectivity against BRD4 bromodomains through structure based rational drug design guided iterative chemical modification endeavoring to discover optimal tail-substituted tetrahydroquinolin derivatives. Moreover, DC-CPin734 showed potent inhibitory activity to AML cell line MV4-11 with an IC50 value of 0.55 ± 0.04 μM, and its cellular on-target effects were further evidenced by c-Myc downregulation results. In summary, DC-CPin734 showing good potency, selectivity and anti AML activity could serve as a potent and selective in vitro and in vivo probe of CBP bromodomain and a promising lead compound for future drug development.
Organic Solvent-Free, Pd(II)-Salan Complex-Catalyzed Synthesis of Biaryls via Suzuki-Miyaura Cross-Coupling in Water and Air
Bunda, Szilvia,Udvardy, Antal,Voronova, Krisztina,Joó, Ferenc
, p. 15486 - 15492 (2019/01/03)
With use of a Pd(II)-sulfosalan complex as a water-soluble catalyst, we have developed an efficient synthesis of biaryls via Suzuki-Miyaura cross-coupling in water under aerobic conditions. The water-insoluble target molecules were isolated by simple filtration in analytical purity after washing with 0.01 M aqueous HCl (20 examples). In most cases, palladium contamination was below 5 ppm considered acceptable for active pharmaceutical ingredients. The established method is scalable, reproducible, and provides biaryl products in isolated yields up to 91%.
Preparation method of pure water printing paper based on bimetallic complex
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Paragraph 0038-0041; 0043-0045, (2018/09/08)
The invention discloses a preparation method of pure water printing paper. 4-(2-pyridyl)benzaldehyde is used as raw materials; an Ir-Eu bimetallic complex with humidity response characteristics is sequentially obtained through oxidization reaction, metal
A Arylheterocycle chirality bcr - abl inhibitor and its preparation method and application
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Paragraph 0046; 0047; 0048, (2016/10/09)
The invention discloses aromatic heterocyclic biphenyl Bcr-Abl inhibitors as well as a preparation method and application thereof. A structural formula of the inhibitors is shown in the specification, wherein in the structural formula, Ar is aromatic heterocycle; R is a mono-substituent or a di-substituent, and the substituent is alkyl or halogen. The series of inhibitors have a certain inhibiting effect on ABL1 kinase in vitro, can inhibit tumor cell proliferation and can be used for preparing antitumor drugs, especially CML (chronic myelocytic leukemia) drugs. The preparation method of the aromatic heterocyclic biphenyl Bcr-Abl inhibitors, which is provided by the invention, has the advantages of easiness in obtainment of raw materials, mild reaction conditions, simplicity in operation of reaction processes and cheap used reagents.
KDM1A INHIBITORS FOR THE TREATMENT OF DISEASE
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Paragraph 0338; 0340; 0522; 0524, (2016/09/26)
Disclosed herein are new compounds and compositions and their application as pharmaceuticals for the treatment of diseases. Methods of inhibition of KDM1A, methods of increasing gamma globin gene expression, and methods to induce differentiation of cancer cells in a human or animal subject are also provided for the treatment of diseases such as acute myelogenous leukemia.
Synthesis and biological evaluation of novel aromatic-heterocyclic biphenyls as potent anti-leukemia agents
Dong, Jinyun,Pan, Xiaoyan,Wang, Jinfeng,Su, Ping,Zhang, Lin,Wei, Fen,Zhang, Jie
, p. 780 - 789 (2015/08/06)
As a continuation to our previous research, twenty-eight aromatic-heterocyclic biphenyls were designed and synthesized as novel Bcr-Abl inhibitors. The title compounds were investigated for their antiproliferative activities against wild K562 cells and Imatinib-resistant K562 cells (K562R). The results indicated that most of them exhibited potent Bcr-Abl inhibition and moderate antiproliferative potency against K562 cells. Furthermore, three compounds 3, 7 and 21 displayed moderate antiproliferative activities against K562R cells. Molecular docking indicated that 3 bound more tightly with Bcr-AblT315I compared to Bcr-AblWT. The higher affinity was consistent with its relatively promising K562R cell growth inhibition. These aromatic-heterocyclic biphenyls could be considered as novel lead compound for optimized as Bcr-AblT315I inhibitors. They provide a good starting point for the further development of novel anti-leukemia agents capable of dealing with clinical acquired resistance against Imatinib.
Benzoimidazole derivatives and pharmaceutical composition comprising the same
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Page/Page column 16; 31-32, (2015/12/17)
Disclosed herein are novel benzoimidazole derivatives functioning as antagonists to vanilloid receptor-1, and a pharmaceutical composition comprising the same. They are useful in preventing or treating pain, acute pain, chronic pain, neuropathic pain, pos
Copper-catalysed regioselective azidation of arenes by C-H activation directed by pyridine
Azad, Chandra S.,Narula, Anudeep K.
, p. 100223 - 100227 (2015/12/04)
A novel and efficient copper-catalysed pyridine directed ortho-azidation of arenes has been developed using safe and stable benzotriazole sulphonyl azide as the azidating agent. A variety of organo azides have been synthesized with electron donor and with
