5392-12-1Relevant academic research and scientific papers
SMALL MOLECULE INHIBITORS OF A PROTEIN COMPLEX
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Paragraph 00178, (2020/12/29)
Compositions and methods for treating thrombosis, inflammation, and atherosclerosis by administration of a compound that binds to KRIT1 to inhibit binding with HEG1.
2, 3-dihydronaphthalo [2, 3-b] furan-4, 9-diketone compound as well as preparation method and application thereof
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Paragraph 0215-0217, (2020/11/05)
The invention provides a 2, 3-dihydronaphthalo [2, 3-b] furan-4, 9-diketone compound as well as a preparation method and application thereof, and belongs to the technical field of medicines. The invention particularly provides the 2, 3-dihydronaphthalo [2, 3-b] furan-4, 9-diketone compounds shown as general formulas I-A and I-B, a pharmaceutical composition containing the compounds, and a preparation method of the compounds. The compound has STAT3 inhibitory activity and can be used for preparing drugs for treating and/or preventing diseases related to STAT3 activity, and the diseases comprisevarious cancers such as breast cancer, lung cancer, oral cancer, kidney cancer, esophageal cancer, liver cancer, stomach cancer, intestinal cancer, cervical cancer and ovarian cancer.
Highly Efficient Microwave-assisted One-Pot Synthesis of Aromatic Nitriles from Aromatic Aldehydes
Pujari,Thorat,Mahipal,Bhondwe
, p. 702 - 706 (2019/07/17)
A highly efficient and environmentally benign protocol is described for the microwave-assisted one-pot synthesis of aromatic nitriles from aromatic aldehydes by the reaction with hydroxylamine hydrochloride in DMSO, which involves the intermediate formation of aldoximes and subsequent dehydration. The developed synthetic methodology can be readily accomplished with various aldehydes containing both electron-donor and electron-acceptor groups, providing excellent yields of the target products in shorter reaction times (1–2 min) compared to previously reported methodologies.
Electrophilic Aromatic Formylation with Difluoro(phenylsulfanyl) methane
Betterley, Nolan M.,Kongsriprapan, Sopanat,Chaturonrutsamee, Suppisak,Deelertpaiboon, Pramchai,Surawatanawong, Panida,Pohmakotr, Manat,Soorukram, Darunee,Reutrakul, Vichai,Kuhakarn, Chutima
, p. 2033 - 2040 (2018/03/21)
Difluoro(phenylsulfanyl)methane (PhSCF 2 H) was found to undergo a reaction with aromatic compounds mediated by SnCl 4, through a thionium intermediate characterized by NMR and TD-DFT analyses, leading to the formation of a mixture of S, S ′-diphenyl dithioacetal and aromatic aldehyde which, after oxidative hydrolysis, provides the aromatic aldehyde in good to excellent yields. The salient feature of the present work is the reaction of activated aromatic compounds containing a deactivating ester functional group, leading to the formylated products in good yields.
Synthesis of pharmacologically important naphthoquinones and anticancer activity of 2-benzyllawsone through DNA topoisomerase-II inhibition
Kumar, Balagani Sathish,Ravi, Kusumoori,Verma, Amit Kumar,Fatima, Kaneez,Hasanain, Mohammad,Singh, Arjun,Sarkar, Jayanta,Luqman, Suaib,Chanda, Debabrata,Negi, Arvind S.
, p. 1364 - 1373 (2017/02/18)
Naphthoquinones are naturally occurring biologically active entities. Practical de novo syntheses of three naphthoquinones i.e. lawsone (1), lapachol (2), and β-lapachone (3b) have been achieved from commercially available starting materials. The conversion of lapachol (2) to β-lapachone (3b) was achieved through p-TSA/Iodine/BF3-etherate mediated regioselective cyclisation. Further, 2-alkyl and 2-benzyllawsone derivatives have been prepared as possible anticancer agents. Four derivatives exhibited significant anticancer activity and the best analogue i.e. compound 21a exhibited potential anticancer activity (IC50?=?5.2?μM) against FaDu cell line. Compound 21a induced apoptosis through activation of caspase pathway and exerted cell cycle arrest at S phase in FaDU cells. It also exhibited significant topoisomerase-II inhibition activity. Compound 21a was found to be safe in Swiss albino mice up to 1000?mg/kg oral dose.
Remarkable Ability of the Benzylidene Ligand To Control Initiation of Hoveyda–Grubbs Metathesis Catalysts
Basak, Tymoteusz,Grudzień, Krzysztof,Barbasiewicz, Micha?
supporting information, p. 3513 - 3523 (2016/07/29)
The structure of the chelating benzylidene ligand offers the unique ability to control the initiation of Hoveyda–Grubbs metathesis catalysts. Apart from steric and electronic effects acting on the step involving opening of the chelate ring, changes related to the following ligand-exchange process may also play a critical role. Our mechanistic model reveals that ligands substituted at the 6-position of the benzylidene ring enter the metathesis cycle in a nonoptimal chelating conformation, and thus the coordination number of the ruthenium center transiently increases to six (associative mechanism). In effect, the synthesis and initiation of the catalysts becomes difficult, and the energy barrier of the ligand-exchange process is controlled by the structure of the coordinating OR group. Moreover, we explain how isomeric naphthalene ligands affect the catalytic performance by an indivisible combination of steric and π-electron delocalization effects.
Naphthyl, (substituted) aryl, piperazine base trunk apperception composition
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Paragraph 0357; 0358, (2016/10/08)
The invention discloses (substituted) naphthyl, (substituted) aryl, piperazinyl amidine compound with new structures and salt of medical acid, a preparation method and a purification method of the compound and the salt of the medical acid, and a medicine composition containing the compound, wherein the compound has double inhibition activities of 5-hydroxytryptamine (5-HT) reuptake and noradrenalin (NE) reuptake, and shows strong depression resistance in animal experiments. The compound can be used for treating tristimania, and can also be used for treating other nervous system diseases related to the 5-HT and the NE.
Time resolved spectroscopic studies on a novel synthesized photo-switchable organic dyad and its nanocomposite form in order to develop light energy conversion devices
Dutta, Gopa,Paul, Abhijit,Yadav, Somnath,Bardhan, Munmun,De, Asish,Chowdhury, Joydeep,Jana, Aindrila,Ganguly, Tapan
, p. 5775 - 5784 (2015/01/30)
UV-vis absorption, steady state and time resolved spectroscopic investigations in pico and nanosecond time domain were made in the different environments on a novel synthesized dyad, 3-(2-methoxynaphthalen-1-yl)-1-(4-methoxyphenyl)prop-2-en-1-one (MNTMA) in its pristine form and when combined with gold (Au) nanoparticles i.e., in its nanocomposite structure. Both steady state and time resolved measurements coupled with the DFT calculations performed by using Gaussian 03 suit of software operated in the linux operating system show that though the dyad exhibits mainly the folded conformation in the ground state but on photoexcitation the nanocomposite form of dyad prefers to be in elongated structure in the excited state indicating its photoswitchable nature. Due to the predominancy of elongated isomeric form of the dyad in the excited state in presence of Au Nps, it appears that the dyad MNTMA may behave as a good light energy converter specially in its nanocomposite form. As larger charge separation rate (kCS ～ 4 × 10 s-1) is found relative to the rate associated with the energy wasting charge recombination processes (kCR ～ 3 × 10s-1) in the nanocomposite form of the dyad, it demonstrates the suitability of constructing the efficient light energy conversion devices with Au-dyad hybrid nanomaterials.
Evaluation of synthetic naphthalene derivatives as novel chemical chaperones that mimic 4-phenylbutyric acid
Mimori, Seisuke,Koshikawa, Yukari,Mashima, Yu,Mitsunaga, Katsuyoshi,Kawada, Koichi,Kaneko, Masayuki,Okuma, Yasunobu,Nomura, Yasuyuki,Murakami, Yasuoki,Kanzaki, Tetsuto,Hamana, Hiroshi
, p. 811 - 814 (2015/02/19)
The chemical chaperone 4-phenylbutyric acid (4-PBA) has potential as an agent for the treatment of neurodegenerative diseases. However, the requirement of high concentrations warrants chemical optimization for clinical use. In this study, novel naphthalene derivatives with a greater chemical chaperone activity than 4-PBA were synthesized with analogy to the benzene ring. All novel compounds showed chemical chaperone activity, and 2 and 5 possessed high activity. In subsequent experiments, the protective effects of the compounds were examined in Parkinson's disease model cells, and low toxicity of 9 and 11 was related to amphiphilic substitution with naphthalene.
Palladium-catalyzed amination of chloromethylnaphthalene and chloromethylanthracene derivatives with various amines
Zhang, Sheng,Wang, Yi,Feng, Xiujuan,Bao, Ming
supporting information; experimental part, p. 5492 - 5495 (2012/05/20)
Palladium-catalyzed amination of chloromethylnaphthalene and chloromethylanthracene derivatives to produce naphthylamines and anthrylamines in satisfactory to good yields has been developed. The unprecedented amination reactions proceeded smoothly under mild conditions in the presence of Pd(PPh3)4 as a catalyst.
