79064-26-9Relevant articles and documents
Regioselective alkylation reaction of purines under microwave irradiation
Ginard, Jaume,Jahani, Daniel,Mur, Nuria,Pujol, Maria Dolors,Vi?as, Miquel,Vinuesa, Arturo
, (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
HETEROCYCLIC NITROGEN-CONTAINING PURINE DERIVATIVES, PHARMACEUTICAL PREPARATIONS CONTAINING THESE DERIVATIVES AND THEIR USE IN NEUROPROTECTION
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Page/Page column 11-12, (2020/08/28)
The invention relates to heterocyclic nitrogen-containing purine derivatives, their use in the medicinal applications and compositions containing these derivatives. New generation of compounds possess selective antineurodegenerative properties on neuronal cells and tissues and can be particularly used in the treatment and prophylaxis of neurodegenerative disease, particularly in the treatment and prophylaxis of Parkinson's disease.
Discovery of N2-(4-Amino-cyclohexyl)-9-cyclopentyl- N6-(4-morpholin-4-ylmethyl-phenyl)- 9H-purine-2,6-diamine as a Potent FLT3 Kinase Inhibitor for Acute Myeloid Leukemia with FLT3 Mutations
Gucky, Tomá?,?ezní?ková, Eva,Rado?ová Muchová, Tereza,Jorda, Radek,Klejová, Zuzana,Malínková, Veronika,Berka, Karel,Bazgier, Václav,Ajani, Haresh,Lep?ík, Martin,Divoky, Vladimír,Kry?tof, Vladimír
, p. 3855 - 3869 (2018/05/14)
FLT3 tyrosine kinase is a potential drug target in acute myeloid leukemia (AML) because patients with FLT3-ITD mutations respond poorly to standard cytotoxic agents and there is a clear link between the disease and the oncogenic properties of FLT3. We present novel 2,6,9-trisubstituted purine derivatives with potent FLT3 inhibitory activity. The lead compound 7d displays nanomolar activity in biochemical assays and selectively blocks proliferation of AML cell lines harboring FLT3-ITD mutations, whereas other transformed and normal human cells are several orders of magnitude less sensitive. The MV4-11 cells treated with 7d suppressed the phosphorylation of FLT3 and its downstream signaling pathways, with subsequent G1 cell cycle arrest and apoptosis. Additionally, a single dose of 7d in mice with subcutaneous MV4-11 xenografts caused sustained inhibition of FLT3 and STAT5 phosphorylation over 48 h, in contrast to the shorter effect observed after administration of the reference FLT3 inhibitor quizartinib.