51264-70-1Relevant academic research and scientific papers
A NIR light-triggered drug delivery system using core-shell gold nanostars-mesoporous silica nanoparticles based on multiphoton absorption photo-dissociation of 2-nitrobenzyl PEG
Hernández-Montoto, Andy,Gorbe, Mónica,Llopis-Lorente, Antoni,Terrés, José Manuel,Montes, Roberto,Cao-Milán, Roberto,Díaz De Gre?u, Borja,Alfonso, María,Orzaez, Mar,Marcos, María Dolores,Martínez-Má?ez, Ramón,Sancenón, Félix
, p. 9039 - 9042 (2019)
Gold nanostars coated with a mesoporous silica shell and functionalized with poly(ethylene glycol) containing photolabile 2-nitrobenzyl moieties are able to release doxorubicin after NIR light irradiation at low power irradiance via a multiphoton absorpti
Curcumin-based fluorescent chemosensor for selective and efficient detection of picric acid
Madhu,Sivakumar
, p. 410 - 415 (2019)
We developed a curcumin-based chemosensor (DCD) for selective and efficient detection of Picric acid (PA). The developed chemosensor DCD exhibit a broad emission band at 516 nm and shows green colour fluorescence in DMSO/H2O solution (8:2, v/v)
3-hydroxycurcumin-4-OCH2CO2H strontium, and synthesis, activity and application thereof
-
Paragraph 0012; 0014-0015, (2020/12/14)
The invention discloses 3-hydroxycurcumin-4-OCH2CO2H strontium, discloses a preparation method of the 3-hydroxycurcumin-4-OCH2CO2H strontium, and discloses anti-osteoporosis activity of the 3-hydroxycurcumin-4-OCH2CO2H strontium so that the invention disc
Targeting receptor tyrosine kinase VEGFR-2 in hepatocellular cancer: Rational design, synthesis and biological evaluation of 1,2-disubstituted benzimidazoles
Abdel-Mohsen, Heba T.,Abdullaziz, Mona A.,Ali, Mamdouh M.,El Diwani, Hoda I.,El Kerdawy, Ahmed M.,Flanagan, Keith J.,Mahmoud, Abeer E. E.,Ragab, Fatma A. F.,Senge, Mathias O.
, (2020/02/26)
In this study, a novel series of 1,2-disubstituted benzo[d]imidazoles was rationally designed as VEGFR-2 inhibitors targeting hepatocellular carcinoma. Our design strategy is twofold; it aimed first at studying the effect of replacing the 5-methylfuryl moiety of the well-known antiangiogenic 2-furylbenzimidazoles with an isopropyl moiety on the VEGFR-2 inhibitory activity and the cytotoxic activity. Our second objective was to further optimize the structures of the benzimidazole derivatives through elongation of the side chains at their one-position for the design of more potent type II-like VEGFR-2 inhibitors. The designed 1,2-disubstituted benzimidazoles demonstrated potent cytotoxic activity against the HepG2 cell line, reaching IC50 = 1.98 μM in comparison to sorafenib (IC50 = 10.99 μM). In addition, the synthesized compounds revealed promising VEGFR-2 inhibitory activity in the HepG2 cell line, e.g., compounds 17a and 6 showed 82% and 80% inhibition, respectively, in comparison to sorafenib (% inhibition = 92%). Studying the effect of 17a on the HepG2 cell cycle demonstrated that 17a arrested the cell cycle at the G2/M phase and induced a dose-dependent apoptotic effect. Molecular docking studies of the synthesized 1,2-disubstituted benzimidazoles in the VEGFR-2 active site displayed their ability to accomplish the essential hydrogen bonding and hydrophobic interactions for optimum inhibitory activity.
Janus Gold Nanostars–Mesoporous Silica Nanoparticles for NIR-Light-Triggered Drug Delivery
Hernández Montoto, Andy,Llopis-Lorente, Antoni,Gorbe, Mónica,M. Terrés, José,Cao-Milán, Roberto,Díaz de Gre?u, Borja,Alfonso, María,Iba?ez, Javier,Marcos, María D.,Orzáez, Mar,Villalonga, Reynaldo,Martínez-Má?ez, Ramón,Sancenón, Félix
, p. 8471 - 8478 (2019/07/16)
Janus gold nanostar–mesoporous silica nanoparticle (AuNSt–MSNP) nanodevices able to release an entrapped payload upon irradiation with near infrared (NIR) light were prepared and characterized. The AuNSt surface was functionalized with a thiolated photolabile molecule (5), whereas the mesoporous silica face was loaded with a model drug (doxorubicin) and capped with proton-responsive benzimidazole-β-cyclodextrin supramolecular gatekeepers (N 1). Upon irradiation with NIR-light, the photolabile compound 5 photodissociated, resulting in the formation of succinic acid, which induced the opening of the gatekeeper and cargo delivery. In the overall mechanism, the gold surface acts as a photochemical transducer capable of transforming the NIR-light input into a chemical messenger (succinic acid) that opens the supramolecular nanovalve. The prepared hybrid nanoparticles were non-cytotoxic to HeLa cells, until they were irradiated with a NIR laser, which led to intracellular doxorubicin release and hyperthermia. This induced a remarkable reduction in HeLa cells viability.
Iridium-catalysed primary alcohol oxidation and hydrogen shuttling for the depolymerisation of lignin
Lancefield, Christopher S.,Teunissen, Lucas W.,Weckhuysen, Bert M.,Bruijnincx, Pieter C. A.
supporting information, p. 3214 - 3221 (2018/07/31)
Lignin is a potentially abundant renewable resource for the production of aromatic chemicals, however its selective depolymerisation is challenging. Here, we report a new catalytic system for the depolymerisation of lignin to novel, non-phenolic monoaromatic products based on the selective β-O-4 primary alcohol dehydrogenation with a Cp?Ir-bipyridonate catalyst complex under basic conditions. We show that this system is capable of promoting the depolymerisation of model compounds and isolated lignins via a sequence of selective primary alcohol dehydrogenation, retro-aldol (Cα-Cβ) bond cleavage and in situ stabilisation of the aldehyde products by transfer (de)hydrogenation to alcohols and carboxylic acids. This method was found to give good to excellent yields of cleavage products with both etherified and free-phenolic lignin model compounds and could be applied to real lignin to generate a range of novel non-phenolic monomers including diols and di-acids. We additionally show, by using the same catalyst in a convergent, one-pot procedure, that these products can be selectively channelled towards a single di-acid product, giving much simpler product mixtures as a result.
Lys modification of curcumin derivatives, their synthesis and use
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Paragraph 0037; 0040; 0041, (2018/11/03)
The present invention discloses pseudo-peptides as the following formula, and further discloses a preparation method and applications of the pseudo-peptides. The pseudo-peptides in the invention have an excellent thrombolytic activity, an antithrombotic a
Pharmacological protection of mitochondrial function mitigates acute limb ischemia/reperfusion injury
Bi, Wei,Bi, Yue,Gao, Xiang,Yan, Xin,Zhang, Yanrong,Harris, Jackie,Legalley, Thomas D.,Gibson, K. Michael,Bi, Lanrong
supporting information, p. 4042 - 4051 (2016/08/01)
We describe several novel curcumin analogues that possess both anti-inflammatory antioxidant properties and thrombolytic activities. The therapeutic efficacy of these curcumin analogues was verified in a mouse ear edema model, a rat arterial thrombosis as
The synthesis and analysis of advanced lignin model polymers
Lancefield,Westwood
supporting information, p. 4980 - 4990 (2015/11/16)
If the lignin-first biorefinery concept becomes a reality, high quality lignins close in structure to native lignins will become available in large quantities. One potential way to utilise this renewable material is through depolymerisation to aromatic chemicals. This will require the development of new chemical methods. Here, we report the synthesis and characterisation of advanced lignin model polymers to be used as tools to develop these methods. The controlled incorporation of the major linkages in lignin is demonstrated to give complex hardwood and softwood lignin model polymers. These polymers have been characterised by 2D HSQC NMR and GPC analysis and have been compared to isolated lignins.
Isolation of functionalized phenolic monomers through selective oxidation and CO bond cleavage of the β-O-4 linkages in Lignin
Lancefield, Christopher S.,Ojo, O. Stephen,Tran, Fanny,Westwood, Nicholas J.
supporting information, p. 258 - 262 (2015/02/19)
Functionalized phenolic monomers have been generated and isolated from an organosolv lignin through a two-step depolymerization process. Chemoselective catalytic oxidation of β-O-4 linkages promoted by the DDQ/tBuONO/ O2 system was achieved in model compounds, including polymeric models and in real lignin. The oxidized β-O-4 linkages were then cleaved on reaction with zinc. Compared to many existing methods, this protocol, which can be achieved in one pot, is highly selective, giving rise to a simple mixture of products that can be readily purified to give pure compounds. The functionality present in these products makes them potentially valuable building blocks.
