- An Activatable Photosensitizer Targeted to γ-Glutamyltranspeptidase
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We adopted a spirocyclization-based strategy to design γ-glutamyl hydroxymethyl selenorhodamine green (gGlu-HMSeR) as a photo-inactive compound that would be specifically cleaved by the tumor-associated enzyme γ-glutamyltranspeptidase (GGT) to generate th
- Chiba, Mayumi,Ichikawa, Yuki,Kamiya, Mako,Komatsu, Toru,Ueno, Tasuku,Hanaoka, Kenjiro,Nagano, Tetsuo,Lange, Norbert,Urano, Yasuteru
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Read Online
- Development of an azo-based photosensitizer activated under mild hypoxia for photodynamic therapy
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Photodynamic therapy (PDT) utilizes photoirradiation in the presence of photosensitizers to ablate cancer cells via generation of singlet oxygen (1O2), but it is important to minimize concomitant injury to normal tissues. One approac
- Piao, Wen,Hanaoka, Kenjiro,Fujisawa, Tomotsumi,Takeuchi, Satoshi,Komatsu, Toru,Ueno, Tasuku,Terai, Takuya,Tahara, Tahei,Nagano, Tetsuo,Urano, Yasuteru
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Read Online
- Synergistic Effects of ppm Levels of Palladium on Natural Clinochlore for Reduction of Nitroarenes
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Augmenting the modified naturally occurring clay clinochlore with ppm amounts of palladium leads to a new and very effective reagent for the reduction of numerous aromatic nitro species. When palladium nanoparticles are supported on pyridyltriazole-modified clinochlore, iron within clinochlore acts synergistically with palladium to catalyze the reduction of a wide variety of nitroarenes at room temperature in aqueous media. Based on E-factor calculations, the catalyst system is found to be in line with green chemistry standards and can be recycled up to five times.
- Gholinejad, Mohammad,Oftadeh, Erfan,Shojafar, Mohammad,Sansano, José M.,Lipshutz, Bruce H.
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p. 4240 - 4248
(2019/09/06)
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- Starch functionalized creatine for stabilization of gold nanoparticles: Efficient heterogeneous catalyst for the reduction of nitroarenes
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Selective reduction of nitroaromatic pollutants into amines with recoverable and reusable heterogeneous catalysts is highly desirable. Herein, we prepared and characterized an efficient novel catalyst comprising 4 nm size Au nanoparticles supported on creatine modified starch. Using this catalyst, efficient reduction of nitroarenes into amines at room temperature in aqueous media was achieved. The presence of creatine in the structure of the catalyst plays important role in amount of Au loading, efficiency of the catalyst, recycling times, and leaching of Au compared to starch supported Au without creatine.
- Gholinejad, Mohammad,Dasvarz, Neda,Shojafar, Mohammad,Sansano, José M.
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- Design, synthesis and biological evaluation of novel 2-phenyl pyrimidine derivatives as potent Bruton's tyrosine kinase (BTK) inhibitors
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BTK is an effective target for the treatment of B-cell malignant tumors and autoimmune diseases. In this work, a series of 2-phenyl pyrimidine derivatives were prepared and their preliminary in vitro activities on B-cell leukemia cells as well as the BTK enzyme were determined. The results showed that compound 11g displayed the best inhibitory activity on BTK with an inhibition rate of 82.76% at 100 nM and excellent anti-proliferation activity on three B-cell leukemia lines (IC50 = 3.66 μM, 6.98 μM, and 5.39 μM against HL60, Raji and Ramos, respectively). Besides, the flow cytometry analysis results indicated that 11g inhibited the proliferation of the Raji cells in a dose- and time-dependent manner, and blocked the Ramos cells at the G0/G1 phase, which is in accordance with the positive control ibrutinib. The mechanism investigation demonstrated that 11g could inhibit the phosphorylation of BTK and its downstream substrate phospholipase γ2 (PLCγ2). All these results showed that 11g was a promising lead compound that merited further optimization as a novel class of BTK inhibitor for the treatment of B-cell lymphoblastic leukemia.
- Li, Xinyu,Shi, Binyu,Teng, Yu,Cheng, Yu,Yang, Huizhu,Li, Jiurong,Wang, Lianjian,He, Siying,You, Qidong,Xiang, Hua
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supporting information
p. 294 - 299
(2019/03/02)
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- 2-phenylpyrimidine compounds, preparation method and medical application
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The invention belongs to the field of medicines and particularly relates to 2-phenylpyrimidine compounds and pharmacologically-acceptable salts thereof and an isotope marker. The invention also discloses a pharmaceutical composition containing the substances and application of the pharmaceutical composition for treating diseases related with protein kinase activity, such as cancer and inflammation. (The formula is shown in the description).
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Paragraph 0098; 0099; 0100; 0101; 0102
(2018/06/15)
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- HYDROGELS WITH BIODEGRADABLE CROSSLINKING
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Hydrogels that degrade under appropriate conditions of pH and temperature by virtue of crosslinking compounds that cleave through an elimination reaction are described. The hydrogels may be used for delivery of various agents, such as pharmaceuticals.
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Paragraph 01
(2017/11/16)
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- TYK2 INHIBITORS AND USES THEREOF
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The present invention provides compounds, compositions thereof, and methods of using the same for the inhibition of TYK2, and the treatment of TYK2-mediated disorders.
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Paragraph 001074; 001075
(2015/09/28)
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- SLOW-RELEASE CONJUGATES OF SN-38
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Conjugates of SN-38 that provide optimal drug release rates and minimize the formation of the corresponding glucuronate are described. The conjugates release SN-38 from a polyethylene glycol through a β-elimination mechanism.
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Paragraph 0059
(2015/04/22)
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- Structure-activity relationship study of non-steroidal NPC1L1 ligands identified through cell-based assay using pharmacological chaperone effect as a readout
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Niemann-Pick type C1-like 1 (NPC1L1) is an intestinal cholesterol transporter that is known to be the target of the cholesterol absorption inhibitor ezetimibe. We previously discovered steroidal NPC1L1 ligands by using a novel cell-based assay that employs pharmacological chaperone effect as a readout. Those steroid derivatives bound to a site different from both the sterol-binding domain and the ezetimibe-binding site, implying that they may be a novel class of NPC1L1 inhibitors with a distinct mode of action. As an extension of that work, we aimed here to find non-steroidal NPC1L1 ligands, which may be better candidates for clinical application than steroidal ligands, by using the same assay to screen our focused library of ligands for liver X receptor (LXR), a nuclear receptor that recognizes oxysterols as endogenous ligands. Here we describe identification of a novel class of NPC1L1 ligands with a ring-fused quinolinone scaffold, and an analysis of the structure-activity relationships of their derivatives as NPC1L1 ligands.
- Karaki, Fumika,Ohgane, Kenji,Fukuda, Hiromitsu,Nakamura, Masahiko,Dodo, Kosuke,Hashimoto, Yuichi
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p. 3587 - 3609
(2014/07/07)
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- Mild and highly selective palladium-catalyzed monoarylation of ammonia enabled by the use of bulky biarylphosphine ligands and palladacycle precatalysts
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A method for the Pd-catalyzed arylation of ammonia with a wide range of aryl and heteroaryl halides, including challenging five-membered heterocyclic substrates, is described. Excellent selectivity for monoarylation of ammonia to primary arylamines was achieved under mild conditions or at rt by the use of bulky biarylphosphine ligands (L6, L7, and L4) as well as their corresponding aminobiphenyl palladacycle precatalysts (3a, 3b, and 3c). As this process requires neither the use of a glovebox nor high pressures of ammonia, it should be widely applicable.
- Cheung, Chi Wai,Surry, David S.,Buchwald, Stephen L.
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supporting information
p. 3734 - 3737
(2013/08/23)
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- SULFONE LINKERS
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Sulfone linkers which couple drugs to carriers of various types are described. These linkers permit the release of the drug over time in a controlled manner. The release occurs through beta-elimination, and does not require enzymatic cleavage. Products of
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Paragraph 0085
(2013/03/26)
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- HYDROGELS WITH BIODEGRADABLE CROSSLINKING
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Hydrogels that degrade under appropriate conditions of pH and temperature by virtue of crosslinking compounds that cleave through an elimination reaction are described. The hydrogels may be used for delivery of various agents, such as pharmaceuticals. Thi
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Paragraph 0114
(2013/03/26)
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- CONTROLLED RELEASE FROM MACROMOLECULAR CONJUGATES
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The invention relates to conjugates of macromolecular carriers and drugs comprising linkers that release the drug or a prodrug through rate-controlled beta-elimination, and methods of making and using the conjugates.
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Page/Page column 44
(2011/11/30)
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- Chemoselective reduction of azides catalyzed by molybdenum xanthate by using phenylsilane as the hydride source
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A chemoselective, neutral, and efficient strategy for the reduction of azides to corresponding amines catalyzed by dioxobis(N,N,-diethyldithiocarbamato) molybdenum complex (1, MoO2[S2CNEt2]2) in the presence of phenylsilane is discovered. This chemoselective reduction strategy tolerates a variety of reducible functional groups.
- Maddani, Mahagundappa R.,Moorthy, Saravana K.,Prabhu, Kandikere R.
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supporting information; experimental part
p. 329 - 333
(2010/03/01)
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- New ammonia equivalents for the Pd-catalyzed amination of aryl halides.
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[reaction: see text]. LiN(SiMe3)2, Ph3SiNH2, and LiNH2 can be be used as ammonia equivalents for the Pd-catalyzed coupling of aryl halides. Using these amine derivatives, simple anilines, including ortho-substituted ones, as well as di- and triarylamines can be readily prepared.
- Huang,Buchwald
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p. 3417 - 3419
(2007/10/03)
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- Method of suppressing body odor with aminobenzoic acid amides
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This invention is directed to a cosmetic deodorant composition comprising: (a) from about 0.1 to 5 percent by weight, based on the weight of the total composition, of aminobenzoic acid amides of the formula STR1 wherein R1 and R2, which may be the same or different, each represent hydrogen, an alkyl of from 1 to 12 carbon atoms; a hydroxyalkyl of from 2 to 4 carbon atoms; an aryl; an aralkyl or carboxyalkyl with from 1 to 3 carbon atoms in the alkyl moiety; or an alkoxyalkyl with from 1 to 8 carbon atoms in the alkoxy moiety and from 1 to 3 carbon atoms in the alkyl moiety, or R1 and R2 together with the amide nitrogen form an optionally substituted heterocyclic ring; and (b) the remainder conventional cosmetic deodorant composition compounds.
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- Studies on Potential Indole Derivatives: Part III-Synthesis and CNS Activity of Some New 1-Substituted-aminomethyl-3--5-substituted-indolin-2-ones
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5-Substituted-indolin-2, 3-diones (1-3) undergo condensation with p-(N,N-diethylcarbamoyl)aniline (4) to give the respective 3--5-substituted-indolin-2-ones (5-7), which on Mannich reaction with different amines furnis
- Srivastava, Neera,Gupta, Anurag Ateet,Gupta, Anil K. Sen
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p. 787 - 789
(2007/10/02)
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