183370-70-9Relevant articles and documents
Influence of 4′-Substitution on the Activity of Gemcitabine and Its ProTide against VZV and SARS-CoV-2
Zheng, Zihua,Groaz, Elisabetta,Snoeck, Robert,De Jonghe, Steven,Herdewijn, Piet,Andrei, Graciela
supporting information, p. 88 - 92 (2020/12/21)
In addition to its therapeutic value as a chemotherapy drug, gemcitabine is of ongoing interest to the scientific community for its broad-spectrum antiviral activity. Herein the synthesis of 4′-methoxy- and 4′-fluoro-substituted gemcitabine analogues along with their phosphoramidate prodrugs is described. Among these derivatives, 4′-fluorogemcitabine proved to be active against varicella zoster virus (VZV, TK+ strain) with an EC50 of 0.042 μM and produced significant cytotoxicity (CC50 = 0.11 μM). Upon derivatization of this trifluoro nucleoside as its prodrug, decreased anti-VZV activity was observed, but with a concomitantly improved selectivity index (SI = 36). When this prodrug was tested against severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), its antiviral activity (EC50 = 0.73 μM) was comparable to or slightly lower than its cytotoxic concentration in measurements of cell growth and cell morphology, respectively.
Radiosynthesis of [18F]-labelled pro-nucleotides (ProtIDes)
Cavaliere, Alessandra,Probst, Katrin C.,Paisey, Stephen J.,Marshall, Christopher,Dheere, Abdul K.H.,Aigbirhio, Franklin,McGuigan, Christopher,Westwell, Andrew D.
, (2020/02/18)
Phosphoramidate pro-nucleotides (ProTides) have revolutionized the field of anti-viral and anti-cancer nucleoside therapy, overcoming the major limitations of nucleoside therapies and achieving clinical and commercial success. Despite the translation of P
Phosphoramidate derivative of nucleoside compound and application thereof
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Paragraph 0207; 0209-0211, (2020/12/30)
The invention belongs to the technical field of medicines, and relates to a phosphoramidate derivative of a nucleoside compound and application thereof, and a pharmaceutical composition containing thecompound. The phosphoramidate derivative can be used as