87818-06-2Relevant academic research and scientific papers
Synthesis and biological evaluation of 6-substituted-5-fluorouridine ProTides
Slusarczyk, Magdalena,Ferla, Salvatore,Brancale, Andrea,McGuigan, Christopher
, p. 551 - 565 (2017/12/28)
A new family of thirteen phosphoramidate prodrugs (ProTides) of different 6-substituted-5-fluorouridine nucleoside analogues were synthesized and evaluated as potential anticancer agents. In addition, antiviral activity against Chikungunya (CHIKV) virus was evaluated using a cytopathic effect inhibition assay. Although a carboxypeptidase Y assay supported a putative mechanism of activation of ProTides built on 5-fluorouridine with such C6-modifications, the Hint docking studies revealed a compromised substrate-activity for the Hint phosphoramidase-type enzyme that is likely responsible for phosphoramidate bioactivation through P–N bond cleavage and free nucleoside 5′-monophosphate delivery. Our observations may support and explain to some extent the poor in vitro biological activity generally demonstrated by the series of 6-substituted-5-fluorouridine phosphoramidates (ProTides) and will be of guidance for the design of novel phosphoramidate prodrugs.
Structure-activity relationships of orotidine-5′-monophosphate decarboxylase inhibitors as anticancer agents
Bello, Angelica M.,Konforte, Danijela,Poduch, Ewa,Furlonger, Caren,Wei, Lianhu,Liu, Yan,Lewis, Melissa,Pai, Emil F.,Paige, Christopher J.,Kotra, Lakshmi P.
experimental part, p. 1648 - 1658 (2010/02/16)
A series of 6-substituted and 5-fluoro-6-substituted uridine derivatives were synthesized and evaluated for their potential as anticancer agents. The designed molecules were synthesized from either fully protected uridine or the corresponding 5-fluorourid
ODCASE INHIBITORS FOR THE TREATMENT OF MALARIA
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Page/Page column 40-41, (2008/06/13)
The present invention includes methods of treating or preventing malaria by administering an anti-malarial effective amount of 6-substituted uridine derivatives to a subject need thereof. The invention also includes new 6-substituted uridine derivatives for use as therapeutics, in particular to treat malaria.
Synthesis and biological activities of 5-substituted 6-phenylthio and 6-iodouridines, a new class of antileukemic nucleosides
Tanaka,Matsuda,Iijima,Hayakawa,Miyasaka
, p. 2164 - 2167 (2007/10/02)
A new class of 5,6-disubstituted uridines, in which the C-6 position was occupied by phenylthio group or iodine, were synthesized via lithiation of the corresponding 5-substituted 2',3'-O-isopropylidene-5'-O-methoxymethyl-uridines and subsequent electroph
