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.
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
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
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
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
Synthesis, antiproliferative, docking and DFT studies of benzimidazole derivatives as EGFR inhibitors
Alam, Mohammad Mahboob,Alzahrani, Hessah Abdullah,Elhenawy, Ahmed A.,Malebari, Azizah M.,Nazreen, Syed
, (2022/01/04)
In the present work, new benzimidazole linked 1,2,3-triazole hybrids have been synthesized and screened for antiproliferative and EGFR kinase inhibitory activities.The structures of these hybrids were elucidated using IR, NMR, mass spectrometry and elemen
BCL-2 INHIBITOR
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Paragraph 0982-0984, (2021/10/22)
Disclosed herein is a compound of Formula (I) for inhibiting both Bcl-2 wild type and mutated Bcl-2, in particular, Bcl-2 G101V and D103Y, and a method of using the compound disclosed herein for treating dysregulated apoptotic diseases.