5651-83-2Relevant articles and documents
"Clicked" bivalent ligands containing curcumin and cholesterol as multifunctional Aβ oligomerization inhibitors: Design, synthesis, and biological characterization
Lenhart, James A.,Ling, Xiao,Gandhi, Ronak,Guo, Tai L.,Gerk, Phillip M.,Brunzell, Darlene H.,Zhang, Shijun
, p. 6198 - 6209 (2010)
In our effort to develop multifunctional compounds that cotarget beta-amyloid oligomers (AβOs), cell membrane/lipid rafts (CM/LR), and oxidative stress, a series of bivalent multifunctional Aβ oligomerization inhibitors (BMAOIs) containing cholesterol and curcumin were designed, synthesized, and biologically characterized as potential treatments for Alzheimer's disease (AD). The in vitro assay results established that the length of spacer that links cholesterol and curcumin and the attaching position of the spacer on curcumin are important structural determinants for their biological activities. Among the BMAOIs tested, 14 with a 21-atom-spacer was identified to localize to the CM/LR of human neuroblastoma MC65 cells, to inhibit the formation of AβOs in MC65 cells, to protect cells from AβOs-induced cytotoxicity, and to retain antioxidant properties of curcumin. Furthermore, 14 was confirmed to have the potential to cross the blood-brain barrier (BBB) as demonstrated in a Caco-2 cell model. Collectively, these results strongly encourage further optimization of 14 as a new hit to develop more potent BMAOIs.
Synthesis and incorporation of a caged tyrosine amino acid possessing a bioorthogonal handle
Padilla, Marshall S.,Farley, Christopher A.,Chatkewitz, Lindsay E.,Young, Douglas D.
, p. 4709 - 4712 (2016)
Reversing a bioconjugation in a spatial and temporal fashion has widespread applications, especially toward targeted drug delivery. We report the synthesis and incorporation of an unnatural amino acid with an alkyne modified dimethoxy-ortho-nitrobenzyl ca
Supramolecular Assembly of Coronene Derivatives for Drug Delivery
Yu, Jie,Chen, Yong,Zhang, Yu-Hui,Xu, Xun,Liu, Yu
, p. 4542 - 4545 (2016)
Possessing a small size and C3-symmetrical rigid backbone, a coronene derivative was synthesized from β-cyclodextrins and hexa-cata-hexabenzocoronene, and then a water-soluble and biocompatible nanographene/polysaccharide supramolecular assembl
Synthesis of Novel 1,2,3-Triazole-dihydro[3,2-c[chromenones as Acetylcholinesterase Inhibitors
Saeedi, Mina,Ansari, Shirin,Mahdavi, Mohammad,Sabourian, Reyhaneh,Akbarzadeh, Tahmineh,Foroumadi, Alireza,Shafiee, Abbas
, p. 2311 - 2318 (2015)
A novel series of 1,2,3-triazole-dihydro[3,2-c]chromenone derivatives were synthesized through an efficient three-step reaction starting from 4-hydroxybenzaldehyde. All the newly synthesized compounds were characterized by infrared and NMR spectroscopy as
Efficient energy transfer between coronene-modified permethyl-β-cyclodextrins and porphyrin for light induced DNA cleavage
Yu, Jie,Zhang, Ying-Ming,Li, Pei-Yu,Liu, Yu
, p. 3717 - 3720 (2017)
A novel supramolecular assembly was constructed by the noncovalent complexation of hexa-cata-hexabenzocoronene modified permethyl-β-cyclodextrins with tetrasodium tetraphenylporphyrintetrasulfonate in water, exhibiting highly efficient excited energy tran
Zinc(ii) triazole: Meso -arylsubstituted porphyrins for UV-visible chloride and bromide detection. Adsorption and catalytic degradation of malachite green dye
Aouadi, Ka?ss,Brahmi, Jihed,Guergueb, Mouhieddinne,Guerineau, Vincent,Loiseau, Frédérique,Najmudin, Shabir,Nasri, Habib,Nasri, Soumaya
, p. 22712 - 22725 (2020)
Three new triazole meso-arylporphyrins (4a-c) were synthesized by the copper(i)-catalyzed azide alkyne cycloaddition (CuAAC) "click"reaction in high yield. The corresponding zinc(ii) coordination compounds (5a-c) have also been prepared. All 4a-c and 5a-c
A Facile Eco-Friendly One-Pot Five-Component Synthesis of Novel 1,2,3-Triazole-Linked Pentasubstituted 1,4-Dihydropyridines and their Biological and Photophysical Studies
Singh, Harjinder,Sindhu, Jayant,Khurana, Jitender M.,Sharma, Chetan,Aneja, Kamal R.
, p. 1088 - 1096 (2013)
An eco-friendly one-pot five-component synthesis of novel 1,2,3-triazole-linked pentasubstituted 1,4-dihydropyridines under ultrasonic and microwave irradiation in polyethylene glycol (PEG) 400 is described. All newly synthesised compounds were evaluated
1,2,3-Triazole tethered β-lactam-Chalcone bifunctional hybrids: Synthesis and anticancer evaluation
Singh, Pardeep,Raj, Raghu,Kumar, Vipan,Mahajan, Mohinder P.,Bedi,Kaur, Tandeep,Saxena
, p. 594 - 600 (2012)
The manuscript describes the synthesis of novel 1,2,3-triazole tethered β-lactam-chalcone bifunctional hybrids via click chemistry approach utilizing azide-alkyne cycloaddition reactions and their evaluation as anticancer agents against four human cancer
Design and synthesis of 1,4-disubstituted 1,2,3-triazoles: Biological evaluation, in silico molecular docking and ADME screening
?e?me, Mustafa,?zgeri?, Fatma Betül,?ahin, ?rfan,Güng?r, ?zge,Tümer, Ferhan
, (2021/09/01)
In this study, propargyl compounds were synthesized from 4-hydroxybenzaldehyde and 3?methoxy-4-hydroxybenzaldehyde (2a-2b). As a result of click reactions of synthesized propargyl compounds (2a-b) with organic azides (4a-4e), carbonyl compounds (5a-5 h) h
Discovery of new 1,4-disubstituted 1,2,3-triazoles: in silico ADME profiling, molecular docking and biological evaluation studies
?e?me, Mustafa,?ahin, ?rfan,Tümer, Ferhan,Yüce, Neslihan
, (2022/01/31)
In this work, eight new 1,2,3-triazoles (6a–h) were synthesized from acetylenes’ “click” reaction with p-substituted azide derivatives. The structures of the compounds were characterized using standard analytical and spectroscopic methods (elemental analy
