Quality Control of Ethyl propiolateIn 2021 ,《First-in-Class Inhibitors of the Ribosomal Oxygenase MINA53》 was published in Journal of Medicinal Chemistry. The article was written by Nowak, Radoslaw P.; Tumber, Anthony; Hendrix, Eline; Ansari, Mohammad Salik Zeya; Sabatino, Manuela; Antonini, Lorenzo; Andrijes, Regina; Salah, Eidarus; Mautone, Nicola; Pellegrini, Francesca Romana; Simelis, Klemensas; Kawamura, Akane; Johansson, Catrine; Passeri, Daniela; Pellicciari, Roberto; Ciogli, Alessia; Del Bufalo, Donatella; Ragno, Rino; Coleman, Mathew L.; Trisciuoglio, Daniela; Mai, Antonello; Oppermann, Udo; Schofield, Christopher J.; Rotili, Dante. The article contains the following contents:
MINA53 is a JmjC domain 2-oxoglutarate-dependent oxygenase that catalyzes ribosomal hydroxylation and is a target of the oncogenic transcription factor c-MYC. Despite its anticancer target potential, no small-mol. MINA53 inhibitors are reported. Using ribosomal substrate fragments, we developed mass spectrometry assays for MINA53 and the related oxygenase NO66. These assays enabled the identification of 2-(aryl)alkylthio-3,4-dihydro-4-oxoypyrimidine-5-carboxylic acids as potent MINA53 inhibitors, with selectivity over NO66 and other JmjC oxygenases. Crystallog. studies with the JmjC demethylase KDM5B revealed active site binding but without direct metal chelation; however, mol. modeling investigations indicated that the inhibitors bind to MINA53 by directly interacting with the iron cofactor. The MINA53 inhibitors manifest evidence for target engagement and selectivity for MINA53 over KDM4-6. The MINA53 inhibitors show antiproliferative activity with solid cancer lines and sensitize cancer cells to conventional chemotherapy, suggesting that further work investigating their potential in combination therapies is warranted. The results came from multiple reactions, including the reaction of Ethyl propiolate(cas: 623-47-2Quality Control of Ethyl propiolate)
Ethyl propiolate(cas: 623-47-2) is a clear colorless to pale yellow liquid that is soluble in ethanol, ether and chloroform. It an important organic chemical raw material and pharmaceutical intermediate. Ethyl propargylate is obtained by oxidation of propargyl alcohol to propargylic acid followed by esterification.Quality Control of Ethyl propiolate
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