129392-84-3Relevant academic research and scientific papers
Synthesis of polystyrene-based random copolymers with balanced number of basic or acidic functional groups
Dimitrov, Ivaylo,Jankova, Katja,Hvilsted, S.. Ren
, p. 2044 - 2052 (2010)
Pairs of polystyrene-based random copolymers with balanced number of pendant basic or acidic groups were synthesized utilizing the template strategy. The same poly[(4hydroxystyrene)-ran-styrene] was used as a template backbone for modification. Two different synthetic approaches for the functionalization were applied. The first one involved direct functionalization of the template backbone through alkylation of the phenolic groups with suitable reagents. The second modification approach was based on "click" chemistry, where the introduction of alkyne groups onto the template backbone was followed by copper-catalyzed 1,3 cycloaddition of aliphatic sulfo-nate- or amine-contaning azides. Both synthetic approaches proved to be highly efficient as evidenced by 1H-NMR analyses. The thermal properties were evaluated by differential scanning calorimetry and thermal gravimetric analyses and were influenced by the type of functionality and the modification method. The ether-linked functional colopymers were thermally more stable than their "clicked" analogues.
'Click' synthesized sterol-based cationic lipids as gene carriers, and the effect of skeletons and headgroups on gene delivery
Sheng, Ruilong,Luo, Ting,Li, Hui,Sun, Jingjing,Wang, Zhao,Cao, Amin
, p. 6366 - 6377 (2013)
In this work, we have successfully prepared a series of new sterol-based cationic lipids (1-4) via an efficient 'Click' chemistry approach. The pDNA binding affinity of these lipids was examined by EB displacement and agarose-gel retardant assay. The average particle sizes and surface charges of the sterol-based cationic lipids/pDNA lipoplexes were analyzed by dynamic laser light scattering instrument (DLS), and the morphologies of the lipoplexes were observed by atomic force microscopy (AFM). The cytotoxicity of the lipids were examined by MTT and LDH assay, and the gene transfection efficiencies of these lipid carriers were investigated by luciferase gene transfection assay in various cell lines. In addition, the intracellular uptake and trafficking/localization behavior of the Cy3-DNA loaded lipoplexes were preliminarily studied by fluorescence microscopy. The results demonstrated that the pDNA loading capacity, lipoplex particle size, zeta potential and morphology of the sterol lipids/pDNA lipoplexes depended largely on the molecular structure factors including sterol-skeletons and headgroups. Furthermore, the sterol-based lipids showed quite different cytotoxicity and gene transfection efficacy in A549 and HeLa cells. Interestingly, it was found that the cholesterol-bearing lipids 1 and 2 showed 7-104 times higher transfection capability than their lithocholate-bearing counterparts 3 and 4 in A549 and HeLa cell lines, suggested that the gene transfection capacity strongly relied on the structure of sterol skeletons. Moreover, the study on the structure-activity relationships of these sterol-based cationic lipid gene carriers provided a possible approach for developing low cytotoxic and high efficient lipid gene carriers by selecting suitable sterol hydrophobes and cationic headgroups.
Orthogonal functionalisation of α-helix mimetics
Barnard, Anna,Long, Kerya,Yeo, David J.,Miles, Jennifer A.,Azzarito, Valeria,Burslem, George M.,Prabhakaran, Panchami,A. Edwards, Thomas,Wilson, Andrew J.
, p. 6794 - 6799 (2014)
α-Helix mediated protein-protein interactions are of major therapeutic importance. As such, the design of inhibitors of this class of interaction is of significant interest. We present methodology to modify N-alkylated aromatic oligoamide α-helix mimetics using 'click' chemistry. The effect is shown to modulate the binding properties of a series of selective p53/hDM2 inhibitors. This journal is the Partner Organisations 2014.
The Mass Spectral Loss of Water from Macrocyclic Amino-ketones
Benz, Herbert,Hesse, Manfred
, p. 1636 - 1648 (1993)
Macrocyclic oxo-lactams containing an N-alkylamino side chain are stable natural products.Their electronimpact mass spectra are characterized by intensive >M - H2O>(1+) signals, the molecular ion signal itself is missing.Under electospray ionization condi
68Ga labeled Erlotinib: A novel PET probe for imaging EGFR over-expressing tumors
Jain, Akanksha,Kameswaran, Mythili,Pandey, Usha,Prabhash, Kumar,Sarma, Haladhar Dev,Dash, Ashutosh
, p. 4552 - 4557 (2017)
Molecular imaging using radiolabeled Tyrosine Kinase Inhibitors (TKI) is a promising strategy for detection and staging of EGFR-positive cancers. A novel analogue of one such TKI, Erlotinib has been developed for PET imaging by derivatizing the parent Erl
Synthesis and biological studies of yohimbine derivatives on human α2C-adrenergic receptors
Mustafa, Suni M.,Bavadekar, Supriya A.,Ma, Guoyi,Moore, Bob M.,Feller, Dennis R.,Miller, Duane D.
, p. 2758 - 2760 (2005)
A series of yohimbine derivatives was synthesized and evaluated for binding affinity at the human α2C-adrenergic receptors expressed in Chinese hamster ovary cells. It has been found that compound 5 shows a higher affinity for α2C-AR than the parent compound yohimbine 1, thereby illustrating that the nature of the linkers affect binding potencies on these receptors.
PYRROLOBENZODIAZEPINE DIMER PRECURSOR AND LIGAND-LINKER CONJUGATE COMPOUND THEREOF
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Paragraph 0201; 0204, (2020/02/18)
The present invention relates to a pyrrolobenzodiazepine dimer prodrug and a ligand-linker conjugate compound thereof, a composition containing these, and therapeutic use thereof particularly as an anticancer drug. The stability of the compounds themselves and the stability thereof in plasma are excellent and the compounds are advantageous in terms of manifestation of toxicity, and thus the compounds are industrially useful in that it is possible to target proliferative diseases such as cancer, to perform a specific treatment, to maximize the drug efficacy, and to minimize the occurrence of side effects.
Azido-Desferrioxamine Siderophores as Functional Click-Chemistry Probes Generated in Culture upon Adding a Diazo-Transfer Reagent
Gotsbacher, Michael P.,Codd, Rachel
, p. 1433 - 1445 (2020/02/27)
This work aimed to undertake the in situ conversion of the terminal amine groups of bacterial desferrioxamine (DFO) siderophores, including desferrioxamine B (DFOB), to azide groups to enable downstream click chemistry. Initial studies trialed a precursor-directed biosynthesis (PDB) approach. Supplementing Streptomyces pilosus culture with blunt-end azido/amine non-native substrates designed to replace 1,5-diaminopentane as the native diamine substrate in the terminal amine position of DFOB did not produce azido-DFOB. Addition of the diazo-transfer reagent imidazole-1-sulfonyl azide hydrogen sulfate to spent S. pilosus medium that had been cultured in the presence of 1,4-diaminobutane, as a viable native substrate to expand the suite of native DFO-type siderophores, successfully generated the cognate suite of azido-DFO analogues. CuI-mediated or strain-promoted CuI-free click chemistry reactions between this minimally processed mixture and the appropriate alkyne-bearing biotin reagents produced the cognate suite of 1,4-disubstituted triazole-linked DFO-biotin compounds as potential molecular probes, detected as FeIII-loaded species. The amine-to-azide transformation of amine-bearing natural products in complex mixtures by the direct addition of a diazo-transfer reagent to deliver functional click chemistry reagents adds to the toolbox for chemical proteomics, chemical biology, and drug discovery.
Modular RNA regulators and methods
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Page/Page column 22-23, (2018/10/30)
This disclosure describes modular miRNA regulator molecules and methods of using modular miRNA regulator molecules. Generally, the modular miRNA regulator molecules include a recognition module and an inhibition module. Generally, the recognition module includes a polynucleotide in which at least a portion of the polynucleotide recognizes at least a portion of a preselected pre-miRNA. Generally, the inhibition module includes a moiety that inhibits nuclease processing of the preselected pre-RNA to a mature RNA.
COMPOSITIONS AND METHODS RELATED TO ANTI-CD19 ANTIBODY DRUG CONJUGATES
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Page/Page column 27; 29, (2017/04/11)
In some aspects, the invention relates to an antibody-drug conjugate, comprising an anti-CD 19 antibody; a linker; and an active agent. The antibody-drug conjugate may comprise a self-immolative group. The linker may comprise an O-substituted oxime, e.g., wherein the oxygen atom of the oxime is substituted with a group that covalently links the oxime to the active agent; and the carbon atom of the oxime is substituted with a group that covalently links the oxime to the antibody.
