1484-26-0Relevant articles and documents
Substituted diarylurea derivative as well as preparation method and application thereof
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Paragraph 0157-0158; 0160, (2021/08/19)
The invention relates to a substituted diarylurea derivative as well as preparation and application thereof. Specifically, the invention discloses a compound with a formula (I) or an optical isomer, a cis-trans-isomer or a pharmaceutically acceptable salt thereof, and a preparation method thereof, wherein the definition of each substituent group in the general formula is described in the specification and claims. The invention further discloses a composition containing the compound and application of the composition. The compound disclosed by the invention has excellent anti-cancer activity on HepG2 liver cancer cells, MGC 803 gastric cancer cells, MCF 7 breast cancer cells and the like, and has a good inhibition effect on the growth of human umbilical vein endothelial cells (HUVEC).
A preparation method of the m-aminophenol
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Paragraph 0014; 0038-0041, (2019/07/08)
The invention belongs to organic synthesis and chemical raw material preparation technology field, in particular to m-aminophenol of preparation method and its intermediate, m-aminophenol of the preparation method, comprises the steps of: (1) dinitrobenzene substituted with benzyl alcohol produced by the reaction of 1 - benzyloxy - 3 - nitrophenyl; (2) 1 - benzyloxy - 3 - nitrobenzene for filtering of the alkaline inorganic salt the substitution reaction of the liquid catalytic hydrogenation generating m-aminophenol; or, 1 - benzyloxy - 3 - nitrophenyl replace alkaline inorganic salt and filtered out of the reaction solution after the recovery of the solvent is soluble in the organic solvent and then re-dissolved in the solution of the, generated by the catalytic hydrogenation of m-aminophenol. Without intermediate separation and purification processes, direct catalytic hydrogenation "one-pot" process for preparing m-aminophenol; then the re-crystallization or reduced pressure distillation purification of m-aminophenol. The method is simple, mild reaction conditions, equipment strength requirement is low, not generate intermediate waste, environment-friendly, high yield, is suitable for industrial generation.
Microballs Containing Ni(0)Pd(0) Nanoparticles for Highly Selective Micellar Catalysis in Water
Bihani, Manisha,Bora, Pranjal P.,Nachtegaal, Maarten,Jasinski, Jacek B.,Plummer, Scott,Gallou, Fabrice,Handa, Sachin
, p. 7520 - 7526 (2019/08/15)
Both Ni(0) complexes and nanoparticles (NPs) are unstable in water, which poses a significant hindrance to their application in aqueous synthetic catalysis. To overcome these barriers, ligated Ni(0) nanoparticles (diameter 1 nm) containing a minimum amount of Pd(0) in the microballs formed of amphiphile PS-750-M are developed and applied in the highly selective carbamate cleavage. Selectivity and functional group tolerance are thoroughly investigated. Control experiments revealed the importance of an individual component of the nanocatalyst. Use of our proline-based amphiphile PS-750-M is critical for achieving microball architecture, the stability of nanoparticles, and desired catalytic activity. Once formed, microballs can be isolated and stored at ambient temperature. Catalyst is thoroughly characterized by X-ray photoelectron spectroscopy, scanning electron microscopy, high-resolution transmission electron microscopy, thermogravimetric analysis, infrared, and cyclic voltammetry. For selective catalysis, zero oxidation state of both Ni and Pd is crucial. On the basis of catalyst characterization and control experiments, the plausible reaction mechanism is proposed.
Novel Deazaflavin Analogues Potently Inhibited Tyrosyl DNA Phosphodiesterase 2 (TDP2) and Strongly Sensitized Cancer Cells toward Treatment with Topoisomerase II (TOP2) Poison Etoposide
Kankanala, Jayakanth,Ribeiro, Carlos J. A.,Kiselev, Evgeny,Ravji, Azhar,Williams, Jessica,Xie, Jiashu,Aihara, Hideki,Pommier, Yves,Wang, Zhengqiang
supporting information, p. 4669 - 4682 (2019/05/17)
Topoisomerase II (TOP2) poisons as anticancer drugs work by trapping TOP2 cleavage complexes (TOP2cc) to generate DNA damage. Repair of such damage by tyrosyl DNA phosphodiesterase 2 (TDP2) could render cancer cells resistant to TOP2 poisons. Inhibiting TDP2, thus, represents an attractive mechanism-based chemosensitization approach. Currently known TDP2 inhibitors lack cellular potency and/or permeability. We report herein two novel subtypes of the deazaflavin TDP2 inhibitor core. By introducing an additional phenyl ring to the N-10 phenyl ring (subtype 11) or to the N-3 site of the deazaflavin scaffold (subtype 12), we have generated novel analogues with considerably improved biochemical potency and/or permeability. Importantly, many analogues of both subtypes, particularly compounds 11a, 11e, 12a, 12b, and 12h, exhibited much stronger cancer cell sensitizing effect than the best previous analogue 4a toward the treatment with etoposide, suggesting that these analogues could serve as effective cellular probes.
Enantioselective Visible-Light-Mediated Formation of 3-Cyclopropylquinolones by Triplet-Sensitized Deracemization
Tr?ster, Andreas,Bauer, Andreas,Jandl, Christian,Bach, Thorsten
supporting information, p. 3538 - 3541 (2019/02/01)
3-Allyl-substituted quinolones undergo a triplet-sensitized di-π-methane rearrangement reaction to the corresponding 3-cyclopropylquinolones upon irradiation with visible light (λ=420 nm). A chiral hydrogen-bonding sensitizer (10 mol %) was shown to promote the reaction enantioselectively (88–96 % yield, 32–55 % ee). Surprisingly, it was found that the enantiodifferentiation does not occur at the state of initial product formation but that it is the result of a deracemization event. The individual parameters that control the distribution of enantiomers in the photostationary state have been identified.
Quinolone-based compounds, formulations, and uses thereof
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Page/Page column 103; 104, (2018/07/02)
Provided herein are quinolone-based compounds that can be used for treatment and/or prevention of malaria and formulations thereof. Also provided herein are methods of treating and/or preventing malaria in a subject by administering a quinolone-based compound or formulation thereof provided herein.
AMINATION AND HYDROXYLATION OF ARYLMETAL COMPOUNDS
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Paragraph 0098; 0134; 0135; 0169, (2018/03/25)
In one aspect, the present disclosure provides methods of preparing a primary or secondary amine and hydroxylated aromatic compounds. In some embodiments, the aromatic compound may be unsubstituted, substituted, or contain one or more heteroatoms within the rings of the aromatic compound. The methods described herein may be carried out without the need for transition metal catalysts or harsh reaction conditions.
Discovery of 2-((4,6-dimethylpyrimidin-2-yl)thio)-N-phenylacetamide derivatives as new potent and selective human sirtuin 2 inhibitors
Yang, Lingling,Ma, Xiaobo,Yuan, Chen,He, Yanying,Li, Ling,Fang, Sha,Xia, Wei,He, Tao,Qian, Shan,Xu, Zhihong,Li, Guobo,Wang, Zhouyu
, p. 230 - 241 (2017/04/19)
Human sirtuin 2 (SIRT2) plays pivotal roles in multiple biological processes such as cell cycle regulation, autophagy, immune and inflammatory responses. Dysregulation of SIRT2 was considered as a main aspect contributing to several human diseases, including cancer. Development of new potent and selective SIRT2 inhibitors is currently desirable, which may provide a new strategy for treatment of related diseases. Herein, a structure-based optimization approach led to new 2-((4,6-dimethylpyrimidin-2-yl)thio)-N-phenylacetamide derivatives as SIRT2 inhibitors. SAR analyses with new synthesized derivatives revealed a number of new potent SIRT2 inhibitors, among which 28e is the most potent inhibitor with an IC50 value of 42?nM. The selectivity analyses found that 28e has a very good selectivity to SIRT2 over SIRT1 and SIRT3. In cellular assays, 28e showed a potent ability to inhibit human breast cancer cell line MCF-7 and increase the acetylation of α-tubulin in a dose-dependent manner. This study will aid further efforts to develop highly potent and selective SIRT2 inhibitors for the treatment of cancer and other related diseases.
Novel SIRT2 protein inhibitor and usage thereof in pharmacy
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Paragraph 0149; 0152, (2017/08/28)
The invention discloses a compound or salt, crystallographic form and solvate compounds of the compound acceptable in pharmacy, and the compound and the salt, crystallographic form, solvate compounds of the compound are shown as formula I, wherein X is selected from the formulas (please see the specifications for the formula); R1 is selected from aryl or ceteroary or substituted aryl or substituted ceteroary or from the formula (please see the specifications for the formula); R2 is selected from the formulas (please see the specifications for the formula); and R3 is selected from halogen or C1-C4 alkyl or C1-C4 alkoxy. The novel compound shown in formula I has the advantages that not only is good inhibitory activity achieved to SIRT2, but also the inhibiting effect is achieved to the tumor, and the novel compound has good pharmaceutical potentiality and provides a novel potential choice for the clinical medicament.
Dibenzothiophene Sulfoximine as an NH3 Surrogate in the Synthesis of Primary Amines by Copper-Catalyzed C?X and C?H Bond Amination
Li, Zhen,Yu, Hao,Bolm, Carsten
supporting information, p. 9532 - 9535 (2017/08/01)
Readily accessible dibenzothiophene sulfoximine is an NH3 surrogate allowing the preparation of free anilines by copper-catalyzed cross-coupling reactions with aryl iodides or amides followed by radical S?N bond cleavage. The one-pot/two-step r
