6421-88-1Relevant academic research and scientific papers
COMPOUNDS TARGETING RNA-BINDING PROTEINS OR RNA-MODIFYING PROTEINS
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, (2021/09/11)
The invention relates to a compound represented by Formula (I): or a pharmaceutically acceptable salt thereof, compositions comprising the same and methods of preparing and using the same. The variables are described herein.
Copper nanoparticles (CuNPs) catalyzed chemoselective reduction of nitroarenes in aqueous medium
Chand, Dillip Kumar,Rai, Randhir
, (2021/08/20)
Abstract: A procedure for practical synthesis of CuNPs from CuSO4·5H2O is established, under appropriate reaction conditions, using rice (Oryza sativa) as an economic source of reducing as well as a stabilizing agent. Optical and microscopic techniques are employed for the characterization of the synthesized CuNPs and the sizes of the particles were found to be in the range of 8 ± 2 nm. The nanoparticles are used as a catalyst for chemoselective reduction of aromatic nitro compounds to corresponding amines under ambient conditions and water as a reaction medium. Graphic abstract: CuNPs are synthesized using hydrolysed rice and used as catalyst for chemoselective reduction of nitroarenes to their corresponding amines in water. [Figure not available: see fulltext.]
INDOLEAMINE 2,3-DIOXYGENASE INHIBITORS AND USE OF SAME IN MEDICINE
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Paragraph 0254-0255; 0257, (2020/11/30)
The present invention relates to a compound represented by formula I, a pharmaceutical composition containing the compound of formula I, a method for inhibiting indoleamine 2,3-dioxygenase, and its use in medicine.
Design, synthesis, and biological evaluation of some novel 4-aminoquinazolines as Pan-PI3K inhibitors
Ding, Huai-Wei,Wang, Shu,Qin, Xiao-Chun,Wang, Jian,Song, Hong-Rui,Zhao, Qing-Chun,Song, Shao-Jiang
, p. 2729 - 2740 (2019/05/17)
A series of 4-aminoquinazolines derivatives containing hydrophilic group were designed and identified as potent Pan-PI3K inhibitors in this study. The results of antiproliferative assays in vitro showed that this series of compounds had strong inhibition of tumor growth, especially compound 7b for MCF-7 cells but weak inhibition to normal cells. PI3K kinase assay showed that 7b had high activity for three PI3K isoforms with the IC50 values of picomole. The western blot assay indicated that 7b could decrease the phospho-Akt (S473) in a dose-dependent manner. Further experiments showed that 7b could induce apoptosis in MCF-7 cells. Four key hydrogen bonding interactions were found in the docking of 7b with PI3K kinase. All these results suggested that 7b is a potent PI3K inhibitor and could be considered as a potential candidate for the development of anticancer agents.
Cu(II)-Mediated N-H and N-Alkyl Aryl Amination and Olefin Aziridination
Munnuri, Sailu,Anugu, Raghunath Reddy,Falck, John R.
supporting information, p. 1926 - 1929 (2019/03/11)
Cu(II)-mediated direct NH2 and NH alkyl aryl aminations and olefin aziridinations are described. These room-temperature, one-pot, environmentally friendly procedures replace costly Rh2 catalysts and, in some instances, display important differences with comparable Rh2- and Fe-supported reactions.
Synthesis and evaluation of novel F-18-labeled pyrimidine derivatives: Potential FAK inhibitors and PET imaging agents for cancer detection
Wang, Dawei,Fang, Yu,Wang, Hang,Xu, Xingyu,Liu, Jianping,Zhang, Huabei
, p. 22388 - 22399 (2017/07/10)
Based on computer-assisted drug design, a series of novel pyrimidine derivatives was successfully synthesized and characterized by 1H NMR, 13C HNMR, and MS spectra. All the new compounds were evaluated for their activity against focal adhesion kinase and showed low IC50 values in comparison with control drugs. In particular, for compound 8i, its IC50 value was 0.060 μM, suggesting its advantage as a focal adhesion kinase inhibitor. To evaluate the potentiality of these compounds as PET imaging agents in cancer detection, compounds 8a, 8c, 8h, and 8i were successively labeled with 18F. The four 18F-labeled pyrimidine derivatives showed appropriate log P values and high stability in physiological saline and mouse plasma. Noticeably, compound [18F]-8a with a 4-methoxyl group at the benzene ring exhibited good in vivo biodistribution data in mice bearing the S180 tumor, which promoted a further microPET imaging study of compound [18F]-8a. The microPET image of [18F-8a] administered into the S180 tumor-bearing mice acquired at 60 min post-injection illustrated that the uptake in S180 tumor was obvious. These results suggested that compound [18F]-8a might be a new probe for PET tumor imaging.
Method for preparing initiating agent monomer containing azobenzene structure
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, (2017/01/17)
The invention discloses an azobenzene compound and a synthesis method thereof.The synthesis method in the technical scheme includes the steps that 4-nitrophenol, halohydrin and potassium hydroxide serve as raw materials to synthesize p-nitrobenzene oxygen alcohol; the p-nitrobenzene oxygen alcohol, iron powder and ammonium chloride are reacted to obtain p-aminophenyl oxygen alcohol; a typical diazo coupling reaction is carried out to obtain solid product 4-acrylic acid (N-methyl amino) ethyl alcohol-4'-aminoethanol-azobenzene; the products, 2-bromoisobutyryl bromide and triethylamine are reacted to obtain the final product 4-acrylic acid (N-methyl amino) ethyl alcohol-4'-bromoisobutyric acid alcohol ester base-azobenzene, and washing and vacuum drying are carried out.The azo compound contains azobenzene photochromic groups, carbon-carbon double bonds and active-tail-end bromine atoms at the same time, can serve as a self-trigger monomer to synthesize branched polymers containing the functional azobenzene structures with the atom transfer radical polymerization (ATRP) method, and has potential application photoresponse polymers.
HETEROARYL COMPOUNDS AND USES THEREOF
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, (2015/07/02)
The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.
Development of a sensitive bioluminogenic probe for imaging highly reactive oxygen species in living rats
Kojima, Ryosuke,Takakura, Hideo,Kamiya, Mako,Kobayashi, Eiji,Komatsu, Toru,Ueno, Tasuku,Terai, Takuya,Hanaoka, Kenjiro,Nagano, Tetsuo,Urano, Yasuteru
supporting information, p. 14768 - 14771 (2016/02/05)
A sensitive bioluminogenic probe for highly reactive oxygen species (hROS), SO3H-APL, was developed based on the concept of dual control of bioluminescence emission by means of bioluminescent enzyme-induced electron transfer (BioLeT) and modulation of cell-membrane permeability. This probe enables non-invasive visualization of physiologically relevant amounts of hROS generated deep inside the body of living rats for the first time. It is expected to serve as a practical analytical tool for investigating a wide range of biological functions of hROS in vivo. The design concept should be applicable to other in vivo bioluminogenic probes. You light up my life: A sensitive bioluminogenic probe for highly reactive oxygen species (hROS) was developed based on the concept of dual control of bioluminescence emission by means of bioluminescent enzyme-induced electron transfer (BioLeT) and modulation of cell-membrane permeability. This probe enables non-invasive visualization of physiologically relevant amounts of hROS generated deep inside the body of living rats.
Deacetylcolchicine deriv.
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Paragraph 0460, (2016/10/08)
Provided are 4-modified colchicine compounds and medicines using the same. Specifically provided are colchicine derivatives represented by general formula (1), salts thereof, and solvates of the same. In general formula (1), R1 is a halogen atom, a hydroxyl group, a nitro group, an amino group, or a mono-, di- or tri-fluoromethyl group; R2, R3 and R4 are each a methoxy group or a hydroxyl group, or alternatively R2 and R3, or R3 and R4 together represent a methylenedioxy group; R5 and R6 may be the same or different and are each a hydrogen atom, a C1-6 alkyl group, an arylalkyl group, a C2-6 alkenyl group, -COR7, -COOR8, -SO2R9, -CONR10R11, or -CSNR12R13, or alternatively R5 and R6 together with the nitrogen atom to which R5 and R6 are bonded may form a three- to seven-membered cyclic amino group; R7 is a C1-6 alkyl group or the like; R8 is a C1-6 alkyl group or the like; R9 is a C1-6 alkyl group or the like; R10 and R11 may be the same or different and are each a hydrogen atom, a C1-6 alkyl group, or the like; and R12 and R13 may be the same or different and are each a hydrogen atom, an alkyl group, or the like.
