Aryl phosphoramidate derivatives of d4T have improved anti-HIV efficacy in tissue culture and may act by the generation of a novel intracellular metabolite
New phosphate derivatives of the anti-HIV nucleoside analogue d4T were prepared as potential membrane-soluble prodrugs of the bioactive free nucleotide. The enhanced antiviral potency and/or reduced cytotoxicity of the derivatives leads to an increase in
McGuigan, Christopher,Cahard, Dominique,Sheeka, Hendrika M.,De Clercq, Erik,Balzarini, Jan
Phosphoramidate derivatives of d4T with improved anti-HIV efficacy retain fullactivity in thymidine kinase-deficient cells
New phosphate derivatives of the anti-HIV nucleoside analogue d4T were prepared as potential membrane-soluble pro-drugs of the bio-active free nucleotide. Some of the derivatives appear to have enhanced antiviral efficacy relative to the parent nucleoside
McGuigan, Christopher,Cahard, Dominique,Sheeka, Hendrika M.,De Clercq, Erik,Balzarini, Jan
One-pot synthesis of aryl phosphoramidate derivatives of AZT/d4T as anti-HIV prodrugs
Arbuzov reaction of aryl phosphorodichloridite with mixture of one equivalent of AZT or d4T and one equivalent of tert-butyl alcohol led to the corresponding AZT/d4T aryl H-phosphonate diesters, and the following reaction of the H-phosphonate diesters wit
Enhancing effects of a mono-bromo substitution at the para position of the phenyl moiety on the metabolism and anti-HIV activity of d4T-phenyl methoxyalaninyl phosphate derivatives
d4T-5'-[p-Bromophenyl methoxyalaninyl phosphate] (d4T-pBPMAP), a novel phenyl phosphate derivative of 2',3'-didehydro-2',3'-dideoxythymidine (d4T) that has an enhanced ability to undergo hydrolysis due to the electron withdrawing properties of its single
Venkatachalam,Tai, Hung-Liang,Vig, Rakesh,Chen, Chun-Lin,Jan, Shyi-Tai,Uckun, Fatih M.
p. 3121 - 3126
(2007/10/03)
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