143773-73-3Relevant academic research and scientific papers
A novel selective mitochondrial-targeted curcumin analog with remarkable cytotoxicity in glioma cells
Shi, Lei,Gao, Li-li,Cai, Shi-zhong,Xiong, Qian-wei,Ma, Zhou-rui
, (2021)
Naturally occurring polyphenol curcumin (4) or demethoxycurcumin (5) and their synthetic derivatives display promising anticancer activities. However, their further development is limited by low bioavailability and poor selectivity. Thus, a mitochondria-targeted compound 14 (DMC-TPP) was prepared in the present study by conjugating a triphenylphosphine moiety to the phenolic hydroxyl group of demethoxycurcumin to enhance its bioavailability and treatment efficacy. The in vitro biological experiments of DMC-TPP showed that it not only displayed higher cytotoxicity as compared with its parent compound 5, but also exhibited superior mitochondria accumulation ability. Glioma cells were more sensitive to DMC-TPP, which inhibited the proliferation of U251 cells with an IC50 of 0.42 μM. The mechanism studies showed that DMC-TPP triggers mitochondria-dependent apoptosis, caused by caspase activation, production of reactive oxygen species (ROS) and decrease of mitochondrial membrane potential (MMP). In addition, DMC-TPP efficiently inhibited cellular thioredoxin reductase, which contributed to its cytotoxicity. Significantly, DMC-TPP delayed tumor progression in a mouse xenograft model of human glioma cancer. Taken together, the potent in vitro and in vivo antitumor activity of DMC-TPP warrant further comprehensive evaluation as a novel anti-glioma agent.
Mitochondrial-targeting curcumin derivative as well as preparation method and medical application thereof
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Paragraph 0089-0092; 0104-0107; 0100-0103; 0115-0118, (2021/07/21)
The invention relates to the field of natural medicines and medicinal chemistry, in particular to a mitochondria-targeting curcumin derivative. The invention also discloses a preparation method of the curcumin derivative and application of the curcumin de
A highly efficient artificial light-harvesting system with two-step sequential energy transfer based on supramolecular self-assembly
Han, Tingting,Hu, Xiao-Yu,Jiao, Jianmin,Qian, Weirui,Shi, Yukun,Sun, Guangping,Wang, Leyong
supporting information, p. 9590 - 9596 (2020/06/05)
A highly efficient artificial light-harvesting system (ALHS) in the aqueous phase with a two-step sequential energy transfer process has been successfully constructed based on the host-guest interaction between a water-soluble pillar[5]arene (WP5) and a b
Preparation of aggregation-induced emission material with light stability
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Paragraph 0052; 0053, (2019/02/27)
The invention discloses a hindered amine light stabilizer with an aggregation-induced emission (AIE) performance and a synthesis method thereof. The hindered amine light stabilizer is formed through steps including a step of ensuring that AIE pyrone deriv
Governing the DNA-binding mode of styryl dyes by the length of their alkyl substituents-from intercalation to major groove binding
Berdnikova, Daria V.,Sosnin, Nikolai I.,Fedorova, Olga A.,Ihmels, Heiko
, p. 545 - 554 (2018/02/07)
A series of monomeric and homodimeric 4-alkoxystyryl(pyridinium) dyes was synthesized and their DNA-binding properties were investigated. We found that the length of the alkyl substituent has a crucial influence on the binding mode of the dyes, although t
Synthesis and comparative studies of phase transition behaviour of new dimeric liquid crystals consisting of dimethyluracil and biphenyl cores
Abdulkarim-Talaq, Mohammad,Srinivasa,Sie-Tiong, Ha,Hariprasad,Guan-Yeow, Yeap
, p. 765 - 772 (2016/04/26)
A new homologous series of mesogens containing 6-amino-1,3-dimethyluracil moiety have been synthesized. The structures of the compounds were characterised by elemental analysis, FT-IR, 1H and 13C NMR spectroscopic techniques. Their m
1,4-naphthoquinone cations as antiplasmodial agents: Hydroxy-, acyloxy-, and alkoxy-substituted analogues
Lu, Xiao,Altharawi, Ali,Gut, Jiri,Rosenthal, Philip J.,Long, Timothy E.
supporting information, p. 1029 - 1033 (2013/02/22)
Cations of hydroxy-substituted 1,4-naphthoquinones were synthesized and evaluated as antiplasmodial agents against Plasmodium falciparum. The atovaquone analogues were found to be inactive as antagonists of parasite growth, which was attributed to ionization of the acidic hydroxyl moiety. Upon modification to an alkoxy substituent, the antiplasmodial activity was restored in the sub-100 nM range. Optimal inhibitors were found to possess IC50 values of 17.4-49.5 nM against heteroresistant P. falciparum W2.
Design of guanidinium porphyrins as potential G-quadruplex ligands
Xu, Hai-Jun,Richard, Philippe,Barbe, Jean-Michel,Gros, Claude P.
, p. 1073 - 1081 (2013/01/15)
We report herein an easy and smooth synthesis of two novel tetra-meso-substituted porphyrins bearing terminal guanidinium functionalities. These two guanidine derivatives are the porphyrin-based analogs of ZnPC, a closely related phthalocyanine-based molecule with four guanidinium arms already reported as an efficient G-quadruplex ligand.
BENT-CORE LC DECORATED GOLD NANOCLUSTERS
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, (2011/04/18)
Novel thiol-terminated bent-core liquid crystals (LCs) are used to decorate gold nanoparticles. Thioacetate or xanthate/xanthogenate functional groups are used to effect the attachment of the LCs to the gold nanoparticles. Such bent-core decorated nanoparticles may be dissolved in bent-core liquid crystal host media to provide polarizable systems which respond quickly to applied electric fields and exhibit other interesting and useful optical and electro-optic behaviour.
Synthesis of 4-[(diethylamino)methyl]-phenol derivatives as novel cholinesterase inhibitors with selectivity towards butyrylcholinesterase
Yu, Liang,Cao, Rihui,Yi, Wei,Yan, Qin,Chen, Zhiyong,Ma, Lin,Peng, Wenlie,Song, Huacan
experimental part, p. 3254 - 3258 (2010/09/04)
A series of novel cholinesterase inhibitors, being composed of 4-[(diethylamino)methyl]-phenoxy and secondary amine which were linked with a different length alkyl chain, were designed and synthesized from the starting material p-hydroxybenzaldehyde. Thes
