35638-19-8Relevant academic research and scientific papers
Preparation and application of three-branch RGD modified brain glioma targeting lipid material
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, (2021/11/03)
The invention discloses a three-branch RGD-modified glioma targeting lipid material which is used for targeted delivery of brain glioma treatment drugs. One end of the novel lipid material is connected with cholesterol extending through polyethylene glycol, and the other end of the novel lipid material is connected with RGD peptide with brain glioma targeting function, and the novel lipid material can be used for integrin receptor α which is highly expressed on the surface of brain capillary endothelial cells and brain glioma cells. v β3 The affinity between the brain glioma is achieved through the affinity between the brain glioma, and the effective concentration of the therapeutic drug to the brain tumor is improved. The novel lipid lipid material can be used for liposome. The prepared paclitaxel liposome has obvious brain targeting property and tumor targeting property, and has wide application prospects.
HEPARAN SULFATE GLYCOMIMETIC COMPOUNDS AND THEIR PHARMACEUTICAL AND COSMECEUTICAL USES
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, (2018/10/19)
The invention relates to dendritic compounds, the use of these compounds as pharmaceuticals, pharmaceutical and cosmeceutical compositions containing the compounds, and methods of treating cancer, inflammation, diabetic nephropathy, neurodegenerative disorders, Niemann-Pick Type C disease, or dermatological conditions.
Multi-arm single-molecular-weight polyethylene glycol and active derivative, preparation and application thereof
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Paragraph 0226; 0227; 0228; 0229; 0230, (2018/11/03)
The invention discloses multi-arm single-molecular-weight polyethylene glycol and an active derivative, preparation and application thereof. The multi-arm single-molecular-weight polyethylene glycol and the reactive derivative thereof are single molecular weight compounds, the application of a high molecular polymer mixture in the prior art is avoided, and the purity of a drug is effectively improved. When applied to drug modification, the multi-arm single-molecular-weight polyethylene glycol and the active derivative thereof can effectively improve the solubility, stability and immunogenicityof the drug, improve the absorption in vivo of the drug, prolong the half-life period of the drug, improve the bioavailability of the drug, enhance the efficacy of the drug, and reduce the toxic andside effects of the drug. Gel formed by the multi-arm single-molecular-weight polyethylene glycol active derivative provided by the invention can be used for preparing a slow release drug, prolongingthe action time of the drug, reducing the frequency of drug administrations, and improving patient compliance.
Tetrahedral DNA conjugates from pentaerythritol-based polyazides
Ponomarenko, Anna I.,Brylev, Vladimir A.,Sapozhnikova, Ksenia A.,Ustinov, Alexey V.,Prokhorenko, Igor A.,Zatsepin, Timofei S.,Korshun, Vladimir A.
, p. 2386 - 2391 (2016/04/26)
Branching points in DNA nanostructures are usually 3- or 4-way junctions maintained by Watson-Crick non-covalent interactions. However, covalently bound DNA stars could improve the diversity, strength and integrity of DNA nanoscale constructions. We report here the convenient synthesis of 3- and 4-fold pentaerythritol-based azides and their use for the assembly of branched conjugates containing the same or different oligonucleotides (ODNs) and/or fluorescent dyes by stoichiometry controlled copper (I) catalyzed azide alkyne cycloaddition (CuAAC) functionalization.
NUCLEOPHILE-TRIGGERED DEGRADBLE MATERIALS AND METHODS OF MAKING AND USING THE SAME
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, (2016/06/28)
Disclosed herein are degradable materials comprising the reaction product of an oxanorbomadiene crosslinker or derivative thereof and a multivalent nucleophile-terminated compound, wherein the reaction product is a degradable elastic solid capable of entraining cargo. Also disclosed herein are degradable materials comprising a polymeric and hyperbranched crosslinked material made with oxanorbomadiene linkage that can be activated for cleavage at a predetermined rate by addition of a nucleophile. Also disclosed herein are methods of making and using the same.
Single-entity heparan sulfate glycomimetic clusters for therapeutic applications
Tyler, Peter C.,Guimond, Scott E.,Turnbull, Jeremy E.,Zubkova, Olga V.
, p. 2718 - 2723 (2015/03/04)
Heparan sulfate (HS) is a highly sulfated glycosaminoglycan with a variety of critical functions in cell signaling and regulation. HS oligosaccharides can mimic or interfere with HS functions in biological systems; however, their exploitation has been hindered by the complexity of their synthesis. Polyvalent displays of small specific HS structures on dendritic cores offer more accessible constructs with potential advantages as therapeutics, but the synthesis of single-entity HS polyvalent compounds has not previously been described. Herein we report the synthesis of a novel targeted library of single-entity glycomimetic clusters capped with varied HS saccharides. They have the ability to mimic longer natural HS saccharides in their inhibition of the Alzheimer's disease (AD) protease BACE-1. We have identified several single-entity HS clusters with IC50 values in the low-nanomolar range. These HS clusters are drug leads for AD and offer a novel framework for the manipulation of heparan sulfate-protein interactions in general.
Antibodies that inhibit metalloproteins
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, (2016/01/09)
An antibody is disclosed which comprises an antigen recognition region which comprises six CDR amino acid sequences selected from the group consisting of SEQ ID NOs: 4-15. Uses thereof are also disclosed.
DENDRITIC CORE COMPOUNDS
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, (2014/06/23)
The invention relates to compounds that are useful for the preparation of dendrimer compounds, the use of these compounds for preparing dendrimers and processes for preparing the compounds.
Multivalent agents containing 1-substituted 2,3,4-trihydroxyphenyl moieties as novel synthetic polyphenols directed against HIV-1
Flores, Aida,Camarasa, Maria Jose,Perez-Perez, Maria Jesus,San-Felix, Ana,Balzarini, Jan,Quesada, Ernesto
, p. 5278 - 5294 (2014/07/08)
The synthesis and the assessment of the anti-HIV activity of a set of molecules inspired by the multivalent structures of some naturally-occurring polyphenols (tannins) are reported. Different multibranched scaffolds have been derived from pentaerythritol as the central core which distribute spatially synthetic polyphenolic subunits based on 1-substituted 2,3,4-trihydroxyphenyl moieties. A tetrapodal compound (13b) bearing four N-(2,3,4-trihydroxyphenyl) amide groups, exhibits remarkable selective activity against HIV-1 with EC 50 values in the micromolar scale, in the same range as those reported for the most representative anti-HIV tannins. Preliminary SAR studies emphasize the importance of the 1-substituted 2,3,4-trihydroxyphenyl moiety, the presence of an amide as the linker and the multivalent architecture of these molecules, since the anti-HIV activity increases with the number of polyphenolic moieties. The data support the interest in synthetic polyphenols and represent a promising starting point for further design and development of selective HIV-1 inhibitors.
Synthesis of branched cores by poly-O-alkylation reaction under phase transfer conditions. A systematic study
Landeros, José M.,Silvestre, Hugo A.,Guadarrama, Patricia
, p. 412 - 419 (2013/04/23)
In the present paper is described a systematic study of poly-O-alkylation reactions of pentaerythritol (PE) and 1,1,1-tris(hydroxymethyl)ethane (TME) by 1,4 Michael addition, under phase transfer catalysis (PTC), considering the effect of: (1) the organophilicity of PTC (three different catalysts were tested), (2) PTC concentration (from catalytic to equimolar conditions), and (3) the regime of addition of reactants coexisting in the aqueous phase of the heterogeneous reaction system. The less organophilic transfer agent showed the best performance on these reactions. In our case, benzyltriethylammonium chloride (TEBAC) gathers the best features. The presence of NaOH as base, promotes the interfacial mechanism and not the bulk one. Out of the optimal range of concentration of NaOH (35-40%), competition between nucleophiles can occur, due to the saturation of the medium. Regarding the regime of addition of reactants, the scenario where NaOH and TEBAC are less time in contact, favors the formation of the desired products. Finally, the deprotection of tert-butyl groups of the poly-O-alkylated compounds is described, to get branched cores with terminal carboxylic acid groups in good yields (90-94%). Spectroscopic properties, such as IR, 1H and 13C NMR, of the synthesized compounds are also described.
