1878-92-8Relevant articles and documents
Synthesis of N-Glycosyl-2-oxindoles by Pd-Catalyzed N-Arylation of 1-Amidosugars
Letribot, Boris,Redjdal, Wafa,Redjdal, Wafa,Benmerad, Belkacem,Le Bideau, Franck,Alami, Mouad,Messaoudi, Samir
supporting information, p. 4201 - 4206 (2020/06/04)
An efficient intramolecular Pd-catalyzed N-arylation of o-iodo-amidosugars for the synthesis of N-glycosylated oxindoles has been reported. The coupling reaction takes place in toluene and involves Pd(OAc)2/RuPhos catalytic systems in the presence of K2CO3. This versatile approach was extended successfully to the synthesis of other N-glycosylated heterocycles.
Synthesis and biological evaluation of new quinoxaline derivatives of ICF01012 as melanoma-targeting probes
El Aissi, Radhia,Liu, Jianrong,Besse, Sophie,Canitrot, Damien,Chavignon, Olivier,Chezal, Jean-Michel,Miot-Noirault, Elisabeth,Moreau, Emmanuel
supporting information, p. 468 - 473 (2014/06/09)
The aim of this study was the synthesis and pharmacokinetic selection of a best melanin-targeting ligand for addressing anticancer agents to pigmented melanoma. Seven quinoxaline carboxamide derivatives were synthesized and radiolabeled with iodine-125. Biodistribution studies of compounds [ 125I]1a-g performed in melanoma-bearing mice tumor showed significant tumor uptake (range 2.43-5.68%ID/g) within 1 h after i.v. injection. Fast clearance of the radioactivity from the nontarget organs mainly via the urinary system gave high tumor-to-blood and tumor-to-muscle ratios. Given its favorable clearance and high tumor-melanoma uptake at 72 h, amide 1d was the most promising melanoma-targeting ligand in this series. Compound 1d will be used as building block for the design of new melanoma-selective drug delivery systems.
COMPOUNDS USEFUL IN THE TREATMENT OF INFLAMMATORY DISEASES
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Page 25, (2010/02/08)
There are provided according to the invention, novel compounds of formula (I)wherein R, R, R, R, Rand Rare as defined in the specification, processes for preparing them, formulations containing them and their use in therapy for the treatment of inflammatory diseases.