21856-53-1Relevant articles and documents
Palladium-Catalyzed Atom-Transfer Radical Cyclization at Remote Unactivated C(sp3)?H Sites: Hydrogen-Atom Transfer of Hybrid Vinyl Palladium Radical Intermediates
Ratushnyy, Maxim,Parasram, Marvin,Wang, Yang,Gevorgyan, Vladimir
supporting information, p. 2712 - 2715 (2018/03/02)
A novel mild, visible-light-induced palladium-catalyzed hydrogen atom translocation/atom-transfer radical cyclization (HAT/ATRC) cascade has been developed. This protocol involves a 1,5-HAT process of previously unknown hybrid vinyl palladium radical intermediates, thus leading to iodomethyl carbo- and heterocyclic structures.
Novel small molecule compounds, preparation method thereof and method for treating/preventing HIV-1 infected aids by using compound
-
Paragraph 0051, (2017/09/26)
The invention provides novel small molecule compounds inhibiting HIV, especially HIV-1 virus infection, a preparation method thereof and a method for inhibiting HIV, especially HIV-1 virus infection, to treat/prevent aids and relevant diseases by using th
Containing difluoro methylene key bridge of the liquid crystal compound and its preparation method and composition
-
Paragraph 0157; 0158; 0159, (2016/10/07)
The invention discloses a liquid crystal compound containing difluoro-methylene key bridge, a preparation method of the liquid crystal compound containing difluoro-methylene key bridge and a composition containing the liquid crystal compound. The liquid c
Using the same hydroxamic acid derivative and HDAC8 inhibitor (by machine translation)
-
Paragraph 0065; 0066, (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.
Indole derivatives and pharmaceutical composition comprising the same for treating or preventing disease related to RAGE
-
Paragraph 0519-0524, (2021/10/25)
A novel indole-based derivative acceptable salt, and manufacturing method thereof including RAGE associated pharmaceutical composition for the prevention or the treatment of disorders the disclosure. Herein a derivative indole-based according to by antagonism in RAGE, nerve cells with the Amyloid-beta peptide loses purpose: a method of fabricating a apparatus move into brain, Alzheimer's disease associated RAGE disease, cerebrovascular dementia, dementia due to damage bean curd, multi blockade dementia, Alzheimer's disease or the like dementia alcoholic or mixed dementia multi blockade and including dementia, pick (pick) bottle, a smartcrew [...] -Jakob (Creutzfeldt-jakob) bottle, that thyroid gland symptoms , bean curd a blade Parkinson (Parkinson) bottle, Huntington's disease (Huntington) which is useful in preventing or treating, can be used.
ITRACONAZOLE ANALOGS AND USE THEREOF
-
Paragraph 0261, (2013/03/26)
Provided herein are Itraconazole analogs. Also provided herein are methods of inhibition of Hedgehog pathway, vascular endothelial growth factor receptor 2 (VEGFR2) glycosylation, angiogenesis and treatment of disease with Itraconazole analogs.
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.
Itraconazole Side Chain Analogues: Structure-Activity Relationship Studies for Inhibition of Endothelial Cell Proliferation, Vascular Endothelial Growth Factor Receptor 2 (VEGFR2) Glycosylation, and Hedgehog Signaling
Shi, Wei,Nacev, Benjamin A.,Aftab, Blake T.,Head, Sarah,Rudin, Charles M.,Liu, Jun O.
supporting information; experimental part, p. 7363 - 7374 (2011/12/04)
Itraconazole is an antifungal drug that was recently found to possess potent antiangiogenic activity and anti-hedgehog (Hh) pathway activity. To search for analogues of itraconazole with greater potency and to understand the structure-activity relationship in both antiangiogenic and Hh targeting activity, 25 itraconazole side chain analogues were synthesized and assayed for inhibition of endothelial cell proliferation and Gli1 transcription in a medulloblastoma (MB) culture. Through this analysis, we have identified analogues with increased potency for inhibiting endothelial cell proliferation and the Hh pathway, as well as VEGFR2 glycosylation that was recently found to be inhibited by itraconazole. An SAR analysis of these activities revealed that potent activity of the analogues against VEGFR2 glycosylation was generally driven by side chains of at least four carbons in composition with branching at the α or β position. SAR trends for targeting the Hh pathway were divergent from those related to HUVEC proliferation or VEGFR2 glycosylation. These results also suggest that modification of the sec-butyl side chain can lead to enhancement of the biological activity of itraconazole.
NOVEL COMPOUNDS AS CANNABINOID RECEPTOR LIGANDS
-
Page/Page column 69, (2010/04/23)
Disclosed herein are cannabinoid receptor ligands of formula (I) wherein A1, A5, Rx, X4, and z are as defined in the specification. Compositions comprising such compounds, and methods for treating conditions and disorders using such compounds and compositions are also disclosed.
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
