385383-48-2Relevant articles and documents
Cationic cyclotriveratrylene-based glycoconjugate and its interaction with fullerene
Feng, Li-Juan,Li, Hui,Chen, Qi,Han, Bao-Hang
, p. 6985 - 6990 (2013)
Fullerenes exhibit interesting biological activities both in vitro and in vivo. However, the low solubility of fullerenes in aqueous media appears to be a major problem for their biological application. To exploit water-soluble macrocyclic host systems to improve the water-solubility of fullerene, a cationic water-soluble CTV derivative containing glucosamine hydrochloride (CTV-GH) is synthesized and well characterized. The supramolecular complexation between CTV-GH and C60 was investigated in organic solvent and aqueous solution, respectively, and confirmed by fluorescence, UV-vis, and Raman spectra. The CTV derivative exhibits a distinct photoluminescence, which can be used to conveniently detect its interaction with C60 through spectrofluorometric titration. CTV-GH can bind C60 in toluene-DMSO solution with the association constant Ka = 4.36 × 10 5 M-1 calculated on the hypothesis of forming a supramolecular complex with 1:1 molar ratio at 298 K. In an aqueous solution, C60 has no absorption intensity due to its insolubility. However, in the presence of CTV-GH, a new characteristic peak of C60 at 342 nm in the UV-vis absorption spectrum was observed for the C60-CTV-GH complex and its intensity greatly increases over 24 h, which proves that CTV-GH can bind C60 in aqueous solution to form a water-soluble complex. The host-guest interaction between sugar-bearing CTV and C60 in aqueous solution will boost the potential biological applications of C60.
Scaffold optimization in discontinuous epitope containing protein mimics of gp120 using smart libraries
Mulder, Gwenn E.,Quarles Van Ufford,Van Ameijde, Jeroen,Brouwer, Arwin J.,Kruijtzer, John A. W.,Liskamp, Rob M. J.
, p. 2676 - 2684 (2013)
A diversity of protein surface discontinuous epitope mimics is now rapidly and efficiently accessible. Despite the important role of protein-protein interactions involving discontinuous epitopes in a wide range of diseases, mimicry of discontinuous epitopes using peptide-based molecules remains a major challenge. Using copper(i) catalyzed azide-alkyne cycloaddition (CuAAC), we have developed a general and efficient method for the synthesis of collections of discontinuous epitope mimics. Up to three different cyclic peptides, representing discontinuous epitopes in HIV-gp120, were conjugated to a selection of scaffold molecules. Variation of the scaffold molecule, optimization of the ring size of the cyclic peptides and screening of the resulting libraries for successful protein mimics led to an HIV gp120 mimic with an IC50 value of 1.7 μM. The approach described here provides rapid and highly reproducible access to clean, smart libraries of very complex bio-molecular constructs representing protein mimics for use as synthetic vaccines and beyond.
APOPTOSIS INHIBITORS
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Paragraph 0381, (2018/02/27)
The invention provides compounds that are inhibitors or covalent modifiers of succinate dehydrogenase subunit B (SDHB) and/or inhibitors of apoptosis, and pharmaceutically acceptable salts, hydrides and stereoisomers thereof. The compounds are employed in pharmaceutical compositions, and methods of making and use, including treating a person in need thereof with an effective amount of the compound or composition.
Total syntheses of three copper (II) tetracarboranylphenylporphyrins containing 40 or 80 boron atoms and their biological properties in EMT-6 tumor-bearing mice
Wu, Haitao,Micca, Peggy L.,Makar, Michael S.,Miura, Michiko
, p. 5083 - 5092 (2008/02/05)
Three carboranyltetraphenylporphyrins containing 40 or 80 boron atoms were synthesized and evaluated for their biodistribution and toxicity in EMT-6 tumor-bearing mice. Copper (II) meso-5,10,15,20-tetrakis[3-methoxy-4-(o-carboranylmethoxy)phenyl]porphyrin
CARBORANYLPORPHYRINS AND USES THEREOF
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Page/Page column 8-9, (2008/06/13)
The present invention is directed to low toxicity boronated compounds and methods for their use in the treatment, visualization, and diagnosis of tumors. More specifically, the present invention is directed to low toxicity carborane-containing 5, 10, 15,