5770-23-0Relevant articles and documents
Synthesis and Pharmacological Evaluation of Identified and Putative Metabolites of the A1 Adenosine Receptor Antagonist 8-Cyclopentyl-3-(3-fluoropropyl)-1-propylxanthine (CPFPX)
Holschbach, Marcus H.,Bier, Dirk,Sihver, Wiebke,Schulze, Annette,Neumaier, Bernd
, p. 770 - 784 (2017/05/26)
The A1 adenosine receptor (A1AR) antagonist [18F]8-cyclopentyl-3-(3-fluoropropyl)-1-propylxanthine ([18F]CPFPX), used in imaging human brain A1ARs by positron emission tomography (PET), is stable in t
Synthesis and evaluation of antitumour activities of novel fused tri-And tetracyclic uracil derivatives
Elkalyoubi, Samar,Fayed, Eman
, p. 771 - 777 (2017/01/03)
Simple one-pot syntheses of indenopyrrolopyrimidines and indolopyrrolopyrimidines were achieved via the cyclocondensation of 6-Aminouracils and, respectively, ninhydrin and isatin in the presence of catalytic amounts of glacial acetic acid. Similarly, 5,6-diaminouracil derivatives were used as starting materials for the synthesis of indenopteridines and indolopteridines via their reaction with ninhydrin and isatin, respectively. The synthesised compounds were evaluated for antitumour activity against a human hepatocellular carcinoma cell line (HepG2), some showing antitumour activity comparable with 5-fluorouracil and imatinib.
Allosteric competitive inhibitors of the glucose-1-phosphate thymidylyltransferase (RmlA) from pseudomonas aeruginosa
Alphey, Magnus S.,Pirrie, Lisa,Torrie, Leah S.,Boulkeroua, Wassila Abdelli,Gardiner, Mary,Sarkar, Aurijit,Maringer, Marko,Oehlmann, Wulf,Brenk, Ruth,Scherman, Michael S.,McNeil, Michael,Rejzek, Martin,Field, Robert A.,Singh, Mahavir,Gray, David,Westwood, Nicholas J.,Naismith, James H.
, p. 387 - 396 (2013/04/24)
Glucose-1-phosphate thymidylyltransferase (RmlA) catalyzes the condensation of glucose-1-phosphate (G1P) with deoxy-thymidine triphosphate (dTTP) to yield dTDP-d-glucose and pyrophosphate. This is the first step in the l-rhamnose biosynthetic pathway. l-R
Structure-based optimization of potent and selective inhibitors of the tyrosine kinase erythropoietin producing human hepatocellular carcinoma receptor B4 (EphB4)
Lafleur, Karine,Huang, Danzhi,Zhou, Ting,Caflisch, Amedeo,Nevado, Cristina
supporting information; experimental part, p. 6433 - 6446 (2010/03/31)
The tyrosine kinase EphB4 is an attractive target for drug design because of its recognized role in cancer-related angiogenesis. Recently, a series of commercially available xanthine derivatives were identified as micromolar inhibitors of EphB4 by high-throughput fragment-based docking into the ATP-binding site of the kinase domain. Here, we have exploited the binding mode obtained by automatic docking for the optimization of these EphB4 inhibitors by chemical synthesis. Addition of only two heavy atoms, methyl and hydroxyl groups, to compound 4 has yielded the single-digit nanomolar inhibitor 66, with a remarkable improvement of the ligand efficiency from 0.26 to 0.37 kcal/(mol per non-hydrogen atom). Compound 66 shows very high affinity for a few other tyrosine kinases with threonine as gatekeeper residue (Abl, Lck, and Src). On the other hand, it is selective against kinases with a larger gatekeeper. A 45 ns molecular dynamics (MD) simulation of the complex of EphB4 and compound 66 provides further validation of the binding mode obtained by fragment-based docking. 2009 American Chemical Society.
Selective, high affinity A2B adenosine receptor antagonists: N-1 monosubstituted 8-(pyrazol-4-yl)xanthines
Kalla, Rao V.,Elzein, Elfatih,Perry, Thao,Li, Xiaofen,Gimbel, Art,Yang, Ming,Zeng, Dewan,Zablocki, Jeff
, p. 1397 - 1401 (2008/09/21)
A series of N-1 monosubstituted 8-pyrazolyl xanthines have been synthesized and evaluated for their affinity for the adenosine receptors (AdoRs). We have discovered two compounds 18 (CVT-7124) and 28 (CVT-6694) that display good affinity for the A2B AdoR (Ki = 6 nM and 7 nM, respectively) and greater selectivity for the human A1, A2A, and A3 AdoRs (>1000-, >830-, and >1500-fold; >850-, >700-, and >1280-fold, respectively). CVT-6694 has been shown to block the release of interleukin-6 and monocyte chemotactic protein-1 from bronchial smooth muscle cells (BSMC), a process believed to be promoted by activation of A2B AdoR.
Synthesis of 3-benzylxanthine and lumazine analogues
El Ashry, El Sayed H.,Youssif, Shaker,El Ahwany, Maged,El Sanan, Mohamed
, p. 262 - 266 (2007/10/03)
Several xanthines (7-13) are prepared by the cyclisation of 1-benzyl-5,6-diaminouracil with single-carbon inserting agents such as aromatic aldehydes, formamides, acetic anhydride, carbon disulfide, and nitrous acid. Treatment of 6-amino-1-benzyl-5-nitros
A2B adenosine receptor antagonists
-
, (2008/06/13)
Disclosed are novel A2B adenosine receptor antagonists having the structure of Formula I or Formula II: The compounds are particularly useful for treating asthma, inflammatory gastrointestinal tract disorders, cardiovascular diseases, neurological disorders, and diseases related to undesirable angiogenesis.
A2B Adenosine receptor antagonists
-
, (2008/06/13)
Disclosed are novel compounds that are A2B adenosine receptor antagonists, useful for treating various disease states, including asthma and diarrhea.
A2B adenosine receptor antagonists
-
, (2008/06/13)
Disclosed are novel A2B adenosine receptor antagonists having the structure of Formula I or Formula II: The compounds are particularly useful for treating asthma, inflammatory gastrointestinal tract disorders, cardiovascular diseases, neurological disorders, and diseases related to undesirable angiogenesis.
XANTHINE DERIVATIVES AS A2B ADENOSINE RECEPTOR ANTAGONISTS
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Page 76-77, (2010/02/09)
Disclosed are compounds that are A2B adenosine receptor antagonists, useful for treating various disease states, including asthma and diarrhea.
