- Highly Efficient Multiple-Labeling Probes for the Visualization of Enzyme Activities
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Quinone methide (QM) as a latent trapping unit has been widely explored in activity-based self-immobilizing reagents. However, further application of this strategy has been largely hampered by the limited labeling efficiency to proteins. In this study, a
- Song, Heng,Li, Yuyao,Chen, Yefeng,Xue, Chenghong,Xie, Hexin
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- First synthesis of tabamides A–C and their derivatives: In vitro nitric oxide inhibitory activity
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The first synthesis of natural phenolic amides, tabamides A–C (1–3), and their derivatives (4–12) was accomplished using Stobbe condensation and amide coupling reactions as key steps. The in vitro nitric oxide (NO) inhibitory effects of these compounds in LPS-induced RAW-264.7 macrophages were evaluated as an indicator of anti-inflammatory activity. All compounds tested had a concentration-dependent inhibitory effect on NO production by RAW-264.7 macrophages without significant cytotoxicity. Compound 6, a tabamide A derivative (IC50 = 82.6 μM), followed by tabamide A (1, IC50 = 100.7 μM), was the most potent from the series. The present study revealed that tabamide A (1) could be considered as a lead structure to develop NO production-targeted anti-inflammatory agents.
- Damodar, Kongara,Shin, Sooyong,Jeon, Sung Ho,Lee, Jeong Tae
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- Facile synthesis of 1,2,3-triazole-fused indolo- and pyrrolo[1,4]diazepines, DNA-binding and evaluation of their anticancer activity
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A facile synthetic strategy has been developed for the generation of structurally diverse N-fused heterocycles. The formation of fused 1,2,3-triazole indolo and pyrrolodiazepines proceeds through an initial Knoevenagel condensation followed by intramolecu
- Gour, Jitendra,Gatadi, Srikanth,Pooladanda, Venkatesh,Ghouse, Shaik Mahammad,Malasala, Satyaveni,Madhavi,Godugu, Chandraiah,Nanduri, Srinivas
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supporting information
(2019/10/05)
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- PHP-Tethered N-Acyl Carbamate: A Photocage for Nicotinamide
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The synthesis of a new photocaged nicotinamide having an N-acyl carbamate linker and a p-hydroxyphenacyl (pHP) chromophore is described. The photophysical and photochemical studies showed an absorption maximum at λ = 330 nm and a quantum yield for release of 11% that are dependent upon both pH and solvent. While the acyl carbamate releases nicotinamide efficiently, a simpler amide linker was inert to photocleavage. This photocaged nicotinamide has significant advantages with respect to quantum yield, absorbance wavelength, rate of release, and solubility that make it the first practical example of a photocaged amide.
- Salahi, Farbod,Purohit, Vatsal,Ferraudi, Guillermo,Stauffacher, Cynthia,Wiest, Olaf,Helquist, Paul
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p. 2547 - 2550
(2018/05/22)
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- Tetrahydro-benzofuran -4 - oxime-based triazole drug, preparation method and application thereof
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The invention relates to a tetrahydrobenzofuran-4-ketoximetriazole medicine. The medicine is a cis-isomeride of tetrahydrobenzofuran-4-ketoximetriazole medicine, and also comprises pharmaceutically acceptable salts and derivatives of the tetrahydrobenzofuran-4-ketoximetriazole medicine. A preparation method of the tetrahydrobenzofuran-4-ketoximetriazole medicine comprises the following steps: preparing 3,6,6-trimethyl-6,7-dihydrobenzofuran-4(5H)-one (intermediate 1) and nitrine (intermediate 2), carrying out a condensation reaction to convert the intermediate 1 into cis-oxime (intermediate 3), separating, purifying, alkylating to obtain propargyl oxime ether (intermediate 4), and carrying out a copper catalyzed cycloaddition reaction on the intermediate 4 and the nitrine (intermediate 2) to synthesize 1,2,3-triazole substituted furocyclohexanone oxime and a derivative thereof. The above compounds have dual curative effects of antiulcer and stomach cancer resistance, and can be used in stomach cancer treatment as alternative medicines.
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- A α - azido carbonyl compound and its preparation method (by machine translation)
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The invention relates to a kind of α - azido carbonyl compound and its preparation method, in organic solvent, in order to end alkyne with trimethyl silicon nitrine as reaction raw material, in the copper catalysts and the persulfate oxidizing agent under the action of the common promotion, through the alkyne of double-functionalized α - azido obtained by reaction of a carbonyl compound. Azido free radical oxidation using air as the oxidizing agent in the terminal played a key role in the reaction process. The method substrate range widely, room temperature operation, mild reaction conditions, after treatment is simple and the yield of the product and high purity, is α - azido carbonyl compound has opened up a new synthetic route and method, and has good application potential and research value. (by machine translation)
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Paragraph 0085; 0086; 0087; 0088; 0089; 0090; 0091-0095
(2017/09/02)
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- A 'photorelease, catch and photorelease' strategy for bioconjugation utilizing a p-hydroxyphenacyl group
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A bioorthogonal 'catch and photorelease' strategy, which combines alkyne-azide cycloaddition between p-hydroxyphenacyl azide and alkyne derivatives to form a 1,2,3-triazole adduct and subsequent photochemical release of the triazole moiety via a photo-Favorskii rearrangement, is introduced. The first step can also involve photorelease of a strained alkyne and its Cu-free click reaction with azide.
- Madea,Slanina,Klán
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supporting information
p. 12901 - 12904
(2016/11/06)
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- Synthesis and cytotoxic activities of 2-substituted (25R)-spirostan-1,4,6-triene-3-ones via ring-opening/elimination and 'click' strategy
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Abstract To develop more effective antitumor steroidal drugs, we synthesized a library including twenty-two novel cytotoxic 2-alkyloxyl substituted (25R)-spirostan-1,4,6-triene-3-ones and corresponding 1,2,3-triazoles through an abnormal monoepoxide ring-opening/elimination and 'click' reactions. After the cytotoxic evaluations against HepG2, Caski and HeLa cell lines, three steroidal triazoles 5b, 5f and 5m in this library were found to possess potent anti-proliferative effects against Caski cells with the half-inhibitory concentrations (IC50) of 9.4-11.8 μM. The high-efficient and straightforward process was attractive feature for facile preparation of anti-tumor steroidal triazoles.
- Lu, Xiao-Feng,Yang, Zheng,Huang, Nian-Yu,He, Hai-Bo,Deng, Wei-Qiao,Zou, Kun
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p. 3726 - 3729
(2015/08/06)
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- Coupling biocatalysis and click chemistry: One-pot two-step convergent synthesis of enantioenriched 1,2,3-triazole-derived diols
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A fully convergent one-pot two-step synthesis of different chiral 1,2,3-triazole-derived diols in high yields and excellent enantio- and diastereoselectivities has been achieved under very mild conditions in aqueous medium by combining a single alcohol dehydrogenase (ADH) with a Cu-catalysed 'click' reaction. The Royal Society of Chemistry 2013.
- Cuetos, Aníbal,Bisogno, Fabricio R.,Lavandera, Iván,Gotor, Vicente
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supporting information
p. 2625 - 2627
(2013/04/23)
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- Biocatalytic deuterium- and hydrogen-transfer using over-expressed ADH-'A': Enhanced stereoselectivity and 2H-labeled chiral alcohols
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Employing the over-expressed highly organic solvent tolerant alcohol dehydrogenase ADH-'A' from Rhodococcus ruber DSM 44541, versatile building blocks, which were not accessible by the wild type catalyst, were obtained in > 99% e.e.; furthermore, employing d8-2-propanol as deuterium source, stereoselective biocatalytic deuterium transfer was made feasible to furnish enantiopure deuterium labeled sec-alcohols on a preparative scale employing a single enzyme. The Royal Society of Chemistry 2006.
- Edegger, Klaus,Gruber, Christian C.,Poessl, Tina M.,Wallner, Sabine R.,Lavandera, Ivan,Faber, Kurt,Niehaus, Frank,Eck, Juergen,Oehrlein, Reinhold,Hafner, Andreas,Kroutil, Wolfgang
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p. 2402 - 2404
(2008/03/28)
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- 7-alkyl- and 7-cycloalkyl-5-aryl-pyrrolo[2,3-d]pyrimidines - Potent inhibitors of the tyrosine kinase c-Src
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7-Substituted-5-aryl-pyrrolo[2,3-d]pyrimidines have been prepared starting from α-bromoacetophenones. These compounds represent a novel class of potent inhibitors of the tyrosine kinase pp60c-Src with good specificity towards other tyrosine kinases (EGF-R, v-Abl).
- Widler, Leo,Green, Jonathan,Missbach, Martin,Susa, Mira,Altmann, Eva
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p. 849 - 852
(2007/10/03)
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