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Deprecated: Implicit conversion from float 245.2 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 ACS+Med+Chem+Lett 2021 ; 12 (1): 88-92 Nephropedia Template TP
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Influence of 4 -Substitution on the Activity of Gemcitabine and Its ProTide Against VZV and SARS-CoV-2 #MMPMID33479570
Zheng Z; Groaz E; Snoeck R; De Jonghe S; Herdewijn P; Andrei G
ACS Med Chem Lett 2021[Jan]; 12 (1): 88-92 PMID33479570show ga
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 EC(50) of 0.042 muM and produced significant cytotoxicity (CC(50) = 0.11 muM). 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 (EC(50) = 0.73 muM) was comparable to or slightly lower than its cytotoxic concentration in measurements of cell growth and cell morphology, respectively.