16855-08-6Relevant articles and documents
Far-red photoactivatable BODIPYs for the super-resolution imaging of live cells
Zhang, Yang,Tang, Sicheng,Ravelo, Laura,Cusido, Janet,Raymo, Fran?isco M.
, p. 131 - 147 (2020)
The identification of viable designs to construct switchable fluorescent probes and operate them in the interior of live cells is essential to allow the acquisition of SMLM images and permit the visualization of cellular components with sub-diffraction resolution. Our laboratories developed a mechanism to switch the fluorescence of BODIPY chromophores with the photoinduced cleavage of oxazine heterocycles under mild 405-nm illumination. With appropriate structural modifications, these switchable molecules can be engineered to immobilize covalently on large biomolecules within lysosomal compartments of live COS-7 cells and produce bright far-red fluorescence with optimal contrast upon activation. Such a combination of properties permits the acquisition of PALM images of the labeled organelles with localization precision of ca. 15 nm. This article reports the experimental protocols for the synthesis of and live-cell labeling with these compounds as well as for the reconstruction of super-resolution images of the resulting biological preparations.
A convenient approach to an advanced intermediate toward the naturally occurring, bioactive 6-substituted 5-hydroxy-4-aryl-1H-quinolin-2-ones
Simonetti, Sebastián O.,Larghi, Enrique L.,Kaufman, Teodoro S.
, p. 2625 - 2636 (2016)
5-Hydroxy-4-aryl-3,4-dihydro-1H-quinolin-2-ones are a small family of natural products isolated from fungal strains of Penicillium and Aspergillus. Most of its members, which are insecticides and anthelmintics, carry an isoprenoid C-6 side chain. The synthesis of a 6-propenyl-substituted advanced intermediate for the total synthesis of these natural products is presented in this paper. This was achieved through the stereoselective construction of a β,β-diarylacrylate derivative from 6-nitrosalicylaldehyde, using a Wittig olefination and a Heck-Matsuda arylation, followed by a selective Fe0-mediated reductive cyclization. Installation of the 6-propenyl side chain was performed by 5-O-allylation of the heterocycle, followed by Claisen rearrangement and conjugative migration of the allyl double bond, as the key steps. The Grubbs II-catalyzed olefin cross metathesis of the 6-allyl moiety with 2-methylbut-2-ene to afford a precursor of peniprequinolone is also reported.
Compound with dual inhibitory activity TDO, IDOO1 and application of compound for treating neurodegenerative disease (by machine translation)
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Paragraph 0172-0175, (2020/10/06)
The present invention provides a compound of formula I, or a pharmaceutically acceptable salt thereof, or a solvate thereof, which can selectively inhibit TDO, IDOO1, which has a significant inhibitory effect on TDO and/or IDOO1. In addition, the prepared compound has a remarkable anti-tumor effect, has a certain treatment effect on's disease and's disease, and has a good application prospect in the field of medicine preparation. (by machine translation)
Co-immobilization of Laccase and TEMPO in the Compartments of Mesoporous Silica for a Green and One-Pot Cascade Synthesis of Coumarins by Knoevenagel Condensation
Mogharabi-Manzari, Mehdi,Amini, Mohsen,Abdollahi, Mohammad,Khoobi, Mehdi,Bagherzadeh, Ghodsieh,Faramarzi, Mohammad Ali
, p. 1542 - 1546 (2018/02/28)
Co-immobilization of bio- and chemocatalysts produces sustainable, recyclable hybrid systems that open new horizons for green cascade approaches in organic synthesis. Here, the co-immobilization of laccase and 2,2,6,6-tetramethylpiperidin-1-oxyl (TEMPO) in mesoporous silica was used for the one-pot aqueous synthesis of 30 coumarin-3-carboxylate derivatives under mild conditions through the condensation of in situ oxidized 2-hydroxybenzyl alcohols and malonate derivatives. A maximum yield was obtained after incubating at pH 6.0 and 45 °C for 24 h. An efficient organic synthesis was catalyzed by the hybrid catalyst in 10 % organic solvent. More than 95 % of the initial activity of the enzyme was preserved after 10 cycles, and no significant catalyst deactivation occurred after 10 runs. This new system efficiently catalyzed the in situ aerobic oxidation of salicyl alcohols, followed by Knoevenagel condensation, which confirmed the possibility of producing efficient hybrid catalysts by co-immobilization of catalytic species in mesoporous materials.
