- Hyperbranched Poly(ester-enamine) from Spontaneous Amino-yne Click Reaction for Stabilization of Gold Nanoparticle Catalysts
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Hyperbranched polymers have garnered much attention due to attractive properties and wide applications, such as drug-controlled release, stimuli-responsive nano-objects, photosensitive materials and catalysts. Herein, two types of novel hyperbranched poly(ester-enamine) (hb-PEEa) were designed and synthesized via the spontaneous amino-yne click reaction of A2 monomer (1, 3-bis(4-piperidyl)-propane (A2a) or piperazine (A2b)) and B3 monomer (trimethylolpropanetripropiolate). According to Flory's hypothesis, gelation is an intrinsic problem in an ideal A2+B3 polymerization system. By controlling the polymerization conditions, such as monomer concentration, molar ratio and rate of addition, a non-ideal A2+B3 polymerization system can be established to avoid gelation and to synthesize soluble hb-PEEa. Due to abundant unreacted alkynyl groups in periphery, the hb-PEEa can be further functionalized by different amino compounds or their derivates. The as-prepared amphiphilic PEG-hb-PEEa copolymer can readily self-assemble into micelles in water, which can be used as surfactant to stabilize Au nanoparticles (AuNPs) during reduction of NaBH4 in aqueous solution. As a demonstration, the as-prepared PEG-hb-PEEa-supported AuNPs demonstrate good dispersion in water, solvent stability and remarkable catalytic activity for reduction of nitrobenzene compounds.
- Yang, Dong,Liu, Pei,Lin, Wanran,Sui, Shanglin,Huang, Long-Biao,Xu, Ben Bin,Kong, Jie
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- Ultrafine NiMoOx nanoparticles confined in mesoporous carbon for the reduction of nitroarenes: effect of the composition and accessibility of the active sites
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The design of ultrafine NiMoOx nanoparticles (NPs) confined in hierarchically porous carbon remains a great challenge due to its high calcination temperature. In addition, the composition of active sites of NiMoOx NPs for the hydrogenation reaction is still ambiguous. Herein, we report a general approach for the synthesis of ultrafine NiMoOx NPs confined in mesoporous carbon with different morphologies and compositions using the replication method with SBA-15 as a hard template. The pore structure of mesoporous carbon and the Ni/Mo composition valence-state were discovered to be the main factors in the reduction of nitroarenes. The NiMoOx/mesoporous carbon-platelet (NiMoOx/MC-PL) with short mesochannels (~350 nm) and high surface area (~995 m2 g?1) possessed excellent catalytic activity towards the reduction of 4-nitrophenol, whereas NiMoOx/mesoporous carbon-hexagonal-prism (NiMoOx/MC-HP), NiMoOx/mesoporous carbon-long-rod (NiMoOx/MC-LR), and NiMoOx/mesoporous carbon-spherical (NiMoOx/MC-SP) with long mesochannels and relatively less surface area exhibited poor catalytic performance. The bifunctional mechanism or electronic synergistic effects of Ni and Mo species enhanced their catalytic performance. A good balance between MoOx and metallic Ni (NiMoOx/MC-PL-450) was found to be suitable for the reduction of 4-NP.
- Li, Shuna,Lv, Yipin,Song, Guolong,Li, Cuncheng,Gao, Daowei,Chen, Guozhu
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- Substituted-3H-imidazo[4,5-c]pyridine and 1H-pyrrolo[2,3-c]pyridine series of novel Ectonucleotide Pyrophosphatase/Phosphodiesterase-1 (ENPP1) and Stimulator for Interferon Genes (STING) modulators as cancer immunotherapeutics
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Substituted -3H-imidazo[4,5-c]pyridine and 1H-pyrrolo[2,3-c]pyridine series of novel Ectonucleotide Pyrophosphatase/Phosphodiesterase-1 (ENPP1) and related compounds, which are useful as inhibitors of ENPP1; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds and compositions to treat disorders associated with dysfunction of the ENPP1.
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Paragraph 0305-0306
(2020/02/19)
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- AMINE-SUBSTITUTED HETEROCYCLIC COMPOUNDS AS EHMT2 INHIBITORS, SALTS THEREOF, AND METHODS OF SYNTHESIS THEREOF
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The present disclosure relates to amine-substituted heterocyclic compounds. The present disclosure also relates to pharmaceutical compositions containing these compounds and methods of treating a disorder (e.g., cancer) by administering an amine-substituted heterocyclic heterocyclic compound disclosed herein or a pharmaceutical composition thereof to subjects in need thereof. The present disclosure also relates to the use of such compounds for research or other non-therapeutic purposes.
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Paragraph 01609
(2019/05/10)
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- NOVEL COMPOUNDS FOR USE IN CANCER
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It relates to the compounds of formula (I), or their pharmaceutically or veterinary acceptable salts, or their stereoisomers or mixtures of stereoisomers, wherein X, L,R1, R 2, and R 3 are as defined herein, which are cancer cell differentiation inducing agents. It also relates to pharmaceutical or veterinary compositions containing them, and to their use in medicine, in particular in the treatment and/or prevention of cancer, in particular by cell differentiation therapy.
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Page/Page column 51
(2019/01/07)
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- Constructing magnetic Si-C-Fe hybrid microspheres for room temperature nitroarenes reduction
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In this work, we present, for the first time, the synthesis and characterization of magnetic Si-C-Fe hybrid microspheres and their catalytic performance in room temperature reduction of 4-nitrophenol as a representative sustainable process for converting environmental pollutants to fine chemicals. The ferrocene-modified polydivinylbenzene (Fc-PDVB) precursor was synthesized by Pt-catalyzed hydrosilylation between the residual vinyl groups on the PDVB surface and 1,1′-bis (dimethylsilyl)ferrocene, where further pyrolysis led to the formation of Fe nanocrystal-containing Si-C-Fe hybrid microspheres. The precursor and hybrid microspheres were characterized by transmission electron microscopy (TEM), Fourier transform infrared spectroscopy (FT-IR), BET surface area/porosity, powder X-ray diffraction (XRD), X-ray photoelectron spectroscopy (XPS), magnetic properties and MAS solid-state NMR measurements. The ultimate microspherical catalyst exhibited nano- and meso-pores, a high specific surface area (i.e., 347.9 m2 g-1) and good ferromagnetic properties. Efficient catalytic activity (TOF: 0.163 s-1), 100% selectivity (to 4-aminophenol) and excellent reusability (with easy separation) have been delivered. The achieved microspheres outperform a number of nanomaterials such as supported noble metal particles, composites, monoliths and sheets. We have confirmed by DFT calculations that the activation of 4-nitrophenol via its weak non-covalent interaction with the sp2 carbon domain of Si-C-Fe hybrid microspheres contributed to the superior performance which can be extended to a range of nitrobenzenes.
- Zhang, Xiaofei,Chen, Lixin,Yun, Jin,Wang, Xiaodong,Kong, Jie
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p. 10986 - 10997
(2017/07/11)
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- NOVEL COMPOUNDS AS DUAL INHIBITORS OF HISTONE METHYLTRANSFERASES AND DNA METHYLTRANSFERASES
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It relates to the use of compounds of formula (I'), or their pharmaceutically or veterinary acceptable salts, or their stereoisomers or mixtures thereof, as anticancer agents and as agents for generating induced pluripotent stem cells. Compounds of formula (I'), wherein R2' is an alcoxy group, a hydrocarbon chain or a ring system, and R1, R3, and R4 are as defined herein, are dual inhibitors of histone methyltransferases and DNA methyltransferases. It also relates to the compounds of formula (I'), or their pharmaceutically or veterinary acceptable salts, or their stereoisomers or mixtures thereof, wherein R2' is phenyl or 5- to 6-membered heteroaromatic ring, both optionally fused to another rings (i.e., compounds of formula (I)). It also relates to pharmaceutical or veterinary compositions containing compounds of formula (I).
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Page/Page column 71-72
(2016/05/09)
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- Synthesis and anticancer activity of 4-aza-daurinol derivatives
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Daurinol, a natural aryl naphthalene lactone, has been reported to have antiproliferative activity against various cell lines, and has also been shown to be efficacious in an in vivo xenograft mouse model. In this study, we tried to discover a new scaffold that enables both rapid structure-activity relationship study of daurinol and scalable synthesis of active compounds. 4-Aza-daurinol, a bioisosterism-based scaffold of daurinol, was designed and 17 analogues were synthesized and evaluated against five representative cancer cell lines. Among them, the 2,3-dihydrobenzo[b][1,4]dioxinyl derivative was found to be the most potent and showed similar activity and tendency as daurinol.
- Hayat, Faisal,Park, Seung-Hyuk,Choi, Nam-Song,Lee, Juyeun,Park, Sung Jean,Shin, Dongyun
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p. 1975 - 1982
(2015/11/24)
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- Highly efficient solvent-free catalytic hydrogenation of solid alkenes and nitro-aromatics using Pd nanoparticles entrapped in aluminum oxy-hydroxide
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Solid alkenes and aromatic nitro compounds are readily hydrogenated to the corresponding alkanes without further reduction of other functional group and amino compounds in nearly quantitative yields in the presence of Pd nanoparticles entrapped in aluminum oxy-hydroxide under the solvent-free condition.
- Chang, Fei,Kim, Hakwon,Lee, Byeongno,Park, Sungho,Park, Jaiwook
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experimental part
p. 4250 - 4252
(2010/09/07)
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- SUBSTITUTED QUINAZOLINE DERIVATIVES AND THEIR USE AS INHIBITORS
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The use of a compound of formula (I) 1 or a salt, ester or amide thereof; where X is O, or S, S(O) or S(O)2, or NR6 where R6 is hydrogen or C1-6 alkyl,; R5 is an optionally substituted 5-membered heteroaromatic ring, R1, R2 ,R3, R4 are independently selected from various specified moieties, in the preparation of a medicament for use in the inhibition of aurora 2 kinase. Certain compounds are novel and these, together with pharmaceutical compositions containing them are also described and claimed
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- Pentafluorobenzenesulfonamides and analogs
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The invention provides methods and compositions relating to novel pentafluorophenylsulfonamide derivatives and analogs and their use as pharmacologically active agents. The compositions find particular use as pharmacological agents in the treatment of disease states, particularly atherosclerosis and hypercholesterolemia, or as lead compounds for the development of such agents. The compositions include compounds of the general formula I: STR1
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- Fiber reactive anthraquinone dyes
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The invention is that of a water soluble fiber reactive anthraquinone blue dyes. These dyes may be used to dye and print textiles and other substrates containing hydroxy and or groups in brilliant blue colors. The dyes of the invention are free of heavy metals.
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- Synthesis of Heptazolidine
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Synthesis of heptazolidine, a carbazole alkaloid from Clausena heptaphylla Wt. and Arn. has been reported to confirm the structure of the alkaloid.
- Roy, Shyamali,Chatterjee, Smarajit K.,Chakraborty, D. P.,Roy, Shyamali
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p. 673 - 675
(2007/10/02)
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