- Towards the development of a targeted albumin-binding radioligand: Synthesis, radiolabelling and preliminary in vivo studies
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Introduction: The compound named 4-[10-(4-(2,5-dioxo-2,5-dihydro-1H-pyrrol-1-yl)butanamido)decyl]-11-[10-(β,D-glucopyranos-1-yl)-1-oxodecyl]-1,4,8,11-tetraazacyclotetradecane-1,8-diacetic acid is a newly synthesised molecule capable of binding in vivo to
- Driver, Cathryn Helena Stanford,Ebenhan, Thomas,Szucs, Zoltan,Parker, Mohammed Iqbal,Zeevaart, Jan Rijn,Hunter, Roger
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- On surface: O -glycosylation by catalytic microcontact printing
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The generation of carbohydrate patterns on surfaces enables a wide range of analytical and diagnostic applications and efficient methods for carbohydrate immobilization are crucial for this purpose. We report on surface O-glycosylation by catalytic printing as a novel, effective method for the covalent immobilization of carbohydrates in micropatterns. Beside the verification of surface functionalization, the suitability of the generated surface for ligand protein interactions was demonstrated.
- Buhl, Moritz,Traboni, Serena,K?rsgen, Martin,Lamping, Sebastian,Arlinghaus, Heinrich F.,Ravoo, Bart Jan
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p. 6203 - 6206
(2017/07/10)
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- RADIOPHARMACEUTICAL CONJUGATE
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This invention relates new radiopharmaceutical conjugates for use in improved methods of diagnosis and treatment of cancer. The radiopharmaceutical conjugate comprises, in sequence: a metabolite that targets tumour cells, bound to a chelating agent capable of containing a radionuclide.bound to a linker capable of binding with an EPR agent in vitro or in vivo; or a chelating agent capable of containing a radionuclide, bound to a metabolite that targets tumour cells, bound to a linker capable of binding with an EPR agent in vitro or in vivo. The radiopharmaceutical conjugates of the present invention provide active and passive targeted radionuclide delivery systems that can help to improve the biodistribution and pharmacological toxicity of the radiopharmaceuticals used for the diagnosis and therapy of cancer.
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- 1,2-Trans-selective synthesis of glycosyl boranophosphates and their utility as building blocks for the synthesis of phosphodiester-linked disaccharides
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Figure Presented A highly 1,2-trans-selective synthesis of glycosyl boranophosphate derivatives by glycosylation of dimethyl boranophosphate with glycosyl iodides was developed. A study on the reaction mechanism indicated that the stereoselectivity of the
- Sato, Kazuki,Oka, Natsuhisa,Fujita, Shoichi,Matsumura, Fumiko,Wada, Takeshi
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experimental part
p. 2147 - 2156
(2010/06/17)
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- Facile preparation of α-glycosyl iodides by in situ generated aluminum iodide: Straightforward synthesis of thio-, seleno-, and o-glycosides from unprotected reducing sugars
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A facile and practical protocol was developed for the synthesis of glycosyl iodides using AlI3 generated in situ from cheap aluminum metal and molecular iodine. Furthermore, in combination with iodine-catalyzed per-O-acetylation, sequential synthesis of per-acetylated glycosyl iodides, per-acetylated thioglycosides, selenoglycoside, and O-glycosides from unprotected reducing sugars was also achieved with complete diastereocontrol in a one-pot version. Supplemental material is available for this article. Go to the publisher's online edition of Journal of Carbohydrate Chemistry to view the free supplemental file. Copyright Taylor & Francis Group, LLC.
- Weng, Shiue-Shien,Li, Chia-Ling,Liao, Chun-Sheng,Chen, Ting-An,Huang, Chao-Cheih,Hung, Kuo-Tung
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experimental part
p. 429 - 440
(2012/06/01)
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- Glycosyl iodides. History and recent advances
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The use of glycosyl iodides as an effective method for the preparation of glycosides has had a recent resurgence in carbohydrate chemistry, despite its early roots in which these species were believed to be of limited use. Renewed interest in these specie
- Meloncelli, Peter J.,Martin, Alan D.,Lowary, Todd L.
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body text
p. 1110 - 1122
(2009/09/05)
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- Stereoselective glycosylations using benzoylated glucosyl halides with inexpensive promoters
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Reactions of O-benzoylated glucopyranosyl halide (I, Br), isolated or generated in situ from per-benzoylated glucose (8a) and trimethylsilyl halide, with various alcohols were efficiently promoted by zinc halide (Cl, Br) or N-bromosuccinimide with a catal
- Murakami, Teiichi,Sato, Yukari,Shibakami, Motonari
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p. 1297 - 1308
(2008/09/21)
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- Contrasting reactivity of thioglucoside and selenoglucoside donors towards promoters: implications for glycosylation stereocontrol
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The stereochemical outcome of glycosylation reactions with model thioglycosides and selenoglycosides proved to be dependent on the source of promoter iodonium ion, with iodine giving different results to N-iodosuccinimide (NIS) alone or N-iodosuccinimide/
- van Well, Renate M.,Kaerkkaeinen, Tiina S.,Kartha, K.P. Ravindranathan,Field, Robert A.
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p. 1391 - 1397
(2007/10/03)
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- Iodine promoted glycosylation with glycosyl iodides: α-glycoside synthesis
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Glycosidation of fully acetylated glucopyranosyl iodide with methanol under the influence of iodine gave α-glucoside selectively. Use of less reactive acceptors led to the formation of α/β-mixtures. Glycosylations with fully benzoylated glucosyl iodide yielded β-glucosides only. In contrast, iodine-promoted glycosylation of serine and threonine with 2-azido-2-deoxy-glycosyl iodides, easily obtained in three steps, proceeded smoothly, resulting in only α-linked products in high yield in most cases. Copyright Taylor & Francis, Inc.
- Van Well, Renate M.,Kartha, K. P. Ravindranathan,Field, Robert A.
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p. 463 - 474
(2007/10/03)
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- Mild synthesis of protected α-D-glycosyl iodides
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α-D-Glycosyl iodides are stereoselectively obtained by iodine replacement of the free anomeric hydroxyl group of fully protected sugars treated with a polymer bound triarylphosphane-iodine complex and imidazole. High yields and mild conditions, compatible
- Caputo, Romualdo,Kunz, Horst,Mastroianni, Domenico,Palumbo, Giovanni,Pedatella, Silvana,Solla, Francesco
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p. 3147 - 3150
(2007/10/03)
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