2346-74-9Relevant articles and documents
Synthesis of N6-[endo-2′-(endo-5′-hydroxy)norbornyl] -8-(N-methylisopropylamino)-9-methyladenine (WRC-0571): A potent and selective adenosine A1 receptor antagonist
Jin, Chunyang,Burgess, Jason P.,Rehder, Kenneth S.,Brine, George A.
, p. 219 - 224 (2007)
A new versatile synthesis of N6-[endo-2′-(endo-5′- hydroxy)norbornyl]-8-(N-methylisopropylamino)-9-methyladenine (WRC-0571), a highly potent and selective antagonist for adenosine A1 receptor, is presented. The overall yield is 14%.
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Barlin,Chapman
, p. 3017,3020 (1965)
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Regioselective alkylation reaction of purines under microwave irradiation
Vinuesa, Arturo,Vi?as, Miquel,Jahani, Daniel,Ginard, Jaume,Mur, Nuria,Pujol, Maria Dolors
, p. 597 - 602 (2021/12/22)
The alkylation of purines which is generally carried out after anion formation by treatment with a base and alkyl halide is complicated and in the best cases, mixtures of N-alkylated compounds are obtained. Purine derivatives can be acquired from alkylati
Synthesis of novel selenotetrazole purine derivatives and their potential chemotherapeutic activities
Dilek, Gulay,Tekin, Ishak Ozel,Coban, Burak,Disli, Ali,Gercek, Zuhal
, p. 84 - 97 (2020/10/08)
The development of novel chemotherapeutic agents is indispensable to improve cancer treatment. One of the conventional approaches toward the synthesis of anticancer agents is the design of a compound whose structure is similar to purines found in DNA. In this study, a series of novel artificial purine nucleosides bearing selenotetrazole pharmacophore, 4a–4h, were synthesized. In order to get preliminary information about their cytotoxic activities, the interaction of compounds with DNA was investigated by UV titration and agarose gel electrophoresis and transcription inhibition studies were performed. The cytotoxic effects of the compounds against B16 melanoma, OV90 ovarian cancer, JM1 lymphoma cell lines, and PHA-induced peripheral blood lymphocytes were also investigated. In cell assay studies, the effects of the compounds on synthesis and mitosis stage of cell cycle were compared by flow cytometry. Although none of the compounds synthesized interacted with DNA and exhibited transcription inhibition, all of them significantly inhibited DNA synthesis phase and showed cytotoxic activity on cancer and proliferating cells. [Figure not available: see fulltext.]
6-Substituted purines as ROCK inhibitors with anti-metastatic activity
Voller, Ji?í,Zahajská, Lenka,Plíhalová, Lucie,Je?ábková, Jana,Burget, David,Pataki, Andreea Csilla,Kry?tof, Vladimír,Zatloukal, Marek,Brábek, Jan,R?sel, Daniel,Mik, Václav,Tká?, Martin,Pospí?il, Tomá?,Gucky, Tomá?,Dole?al, Karel,Strnad, Miroslav
, (2019/07/03)
Rho-associated serine/threonine kinases (ROCKs) are principal regulators of the actin cytoskeleton that regulate the contractility, shape, motility, and invasion of cells. We explored the relationships between structure and anti-ROCK2 activity in a group