795-63-1Relevant academic research and scientific papers
Enhanced photodynamic therapy through supramolecular photosensitizers with an adamantyl-functionalized porphyrin and a cyclodextrin dimer
Xia, Lei,Wu, Jian,Huang, Baoxuan,Gao, Yun,Tian, Jia,Zhang, Weian
supporting information, p. 11134 - 11137 (2020/10/05)
A supramolecular photosensitizer was constructed using a tetra-adamantane-functionalized porphyrin and a dimer of permethyl-β-cyclodextrin through host-guest interaction and self-assembly. The porphyrin/cyclodextrin alternating structure of supramolecular
Wavelength conversion of light stability chromophor
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Paragraph 0245; 0249, (2016/10/08)
The invention provides highly fluorescent materials comprising a single (i=0) or a series (i=1, 2, etc.) of heterocyclic systems. The chromophores are particularly useful for absorption and emission of photons in the visible and near infrared wavelength range. The photo-stable highly luminescent chromophores are useful in various applications, including in wavelength conversion films. Wavelength conversion films have the potential to significantly enhance the solar harvesting efficiency of photovoltaic or solar cell devices.
Using the same hydroxamic acid derivative and HDAC8 inhibitor (by machine translation)
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Paragraph 0066; 0068, (2016/10/09)
Disclosed are: a compound which is capable of inhibiting the function of HDAC8; and an HDAC8 inhibitor. Specifically disclosed is a hydroxamic acid derivative which is characterized by being composed of a compound represented by general formula (1) (wherein X represents an aromatic substituent or an optionally substituted 3-8 membered ring, and n represents an integer of 0-20), or a pharmaceutically acceptable salt, hydrate, solvate or prodrug thereof.
Rapid discovery of highly potent and selective inhibitors of histone deacetylase 8 using click chemistry to generate candidate libraries
Suzuki, Takayoshi,Ota, Yosuke,Ri, Masaki,Bando, Masashige,Gotoh, Aogu,Itoh, Yukihiro,Tsumoto, Hiroki,Tatum, Prima R.,Mizukami, Tamio,Nakagawa, Hidehiko,Iida, Shinsuke,Ueda, Ryuzo,Shirahige, Katsuhiko,Miyata, Naoki
, p. 9562 - 9575 (2013/01/16)
To find HDAC8-selective inhibitors, we designed a library of HDAC inhibitor candidates, each containing a zinc-binding group that coordinates with the active-site zinc ion, linked via a triazole moiety to a capping structure that interacts with residues on the rim of the active site. These compounds were synthesized by using click chemistry. Screening identified HDAC8-selective inhibitors including C149 (IC50 = 0.070 μM), which was more potent than PCI-34058 (6) (IC50 = 0.31 μM), a known HDAC8 inhibitor. Molecular modeling suggested that the phenylthiomethyl group of C149 binds to a unique hydrophobic pocket of HDAC8, and the orientation of the phenylthiomethyl and hydroxamate moieties (fixed by the triazole moiety) is important for the potency and selectivity. The inhibitors caused selective acetylation of cohesin in cells and exerted growth-inhibitory effects on T-cell lymphoma and neuroblastoma cells (GI50 = 3-80 μM). These findings suggest that HDAC8-selective inhibitors have potential as anticancer agents.
First selective CYP11B1 inhibitors for the treatment of cortisol-dependent diseases
Hille, Ulrike E.,Zimmer, Christina,Vock, Carsten A.,Hartmann, Rolf W.
supporting information; experimental part, p. 2 - 6 (2011/04/17)
Outgoing from an etomidate-based design concept, we succeeded in the development of a series of highly active and selective inhibitors of CYP11B1, the key enzyme of cortisol biosynthesis, as potential drugs for the treatment of Cushing's syndrome and rela
Selection of the biological activity of DNJ neoglycoconjugates through click length variation of the side chain
Ardes-Guisot, Nicolas,Alonzi, Dominic S.,Reinkensmeier, Gabriele,Butters, Terry D.,Norez, Caroline,Becq, Frederic,Shimada, Yousuke,Nakagawa, Shinpei,Kato, Atsushi,Bleriot, Yves,Sollogoub, Matthieu,Vauzeilles, Boris
supporting information; experimental part, p. 5373 - 5388 (2011/08/22)
A series of neoglycoconjugates derived from deoxynojirimycin has been prepared by click connection with functionalised adamantanes. They have been assayed as glycosidase inhibitors, as inhibitors of the glycoenzymes relevant to the treatment of Gaucher disease, as well as correctors of the defective ion-transport protein involved in cystic fibrosis. We have demonstrated that it is possible to selectively either strongly inhibit ER-α-glucosidases and ceramide glucosyltransferase or restore the activity of CFTR in CF-KM4 cells by varying the length of the alkyl chain linking DNJ and adamantane.
An unexpected example of protein-templated click chemistry
Suzuki, Takayoshi,Ota, Yosuke,Kasuya, Yuki,Mutsuga, Motoh,Kawamura, Yoko,Tsumoto, Hiroki,Nakagawa, Hidehiko,Finn,Miyata, Naoki
supporting information; experimental part, p. 6817 - 6820 (2010/12/19)
(Figure Presented) It all happened with a click: In a search for histone deacetylase (HDAC) inhibitors using in situ click chemistry, the first example of protein-Cu acceleration of the azide-alkyne cycloaddition reaction was uncovered. The copper center
Carbon-14 labeling of Saxagliptin (BMS-477118)
Cao, Kai,Bonacorsi Jr., Samuel J.,Balasubramanian, Balu,Hanson, Ronald L.,Manchand, Percy,Godfrey Jr., Jollie D.,Fox, Rita,Christopher, Lisa J.,Su, Hong,Iyer, Ramaswamy
, p. 1224 - 1229 (2008/04/05)
An efficient synthesis of carbon-14-labeled Saxagliptin (BMS-477118) is described. Initial synthesis of the key radiolabeled intermediate (S)-N-Boc-2-(3′-hydroxyadamantyl)glycine 2a utilized adamantanemethanol in a 10-step sequence. To shorten the sequenc
