- Design and synthesis of lipophilic phosphoramidate d4T-MP prodrugs expressing high potency against HIV in cell culture: Structural determinants for in vitro activity and QSAR
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A series of new substituted-aryl phosphoramidate derivatives of the anti-HIV drug d4T were synthesized as membrane-soluble nucleotide prodrugs, to extend and quantify the SAR observed for an earlier series of related derivatives. All of the compounds were
- Siddiqui, Adam Q.,McGuigan, Christopher,Ballatore, Carlo,Zuccotto, Fabio,Gilbert, Ian H.,De Clercq, Erik,Balzarini, Jan
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- Large-scale synthesis and formulation of GMP-grade stampidine, a new anti-HIV agent
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The arylphosphoramidate derivative of stavudine (STV, d4T, 2',3'-didehydro-3'-deoxythymidine, CAS 3056-17-5), stampidine (STAMP, DDE-113, HI-113, N-[p-(4-bromophenyl)-2',3'-didehydro-3'-deoxy-5'-thymidylyl]-L-alanine methyl ester, CAS 217178-62-6), is a n
- DuMez, Darin,Venkatachalam, Taracad K.,Uckun, Fatih M.
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p. 136 - 151
(2007/10/03)
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- Synthesis, separation and anti-HIV activity of distereoisomers of N-[p-(4-bromophenyl)-2',3'-didehydro-3'-deoxy-5'-thymidylyl]-L-alanine methyl ester (stampidine)
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The distereoisomers of stampidine (STAMP, DDE-113, HI-113, N-[p-(4-bromophenyi)-2',3'-didehydro-3'-deoxy-5'-thymidylyl]-L-alanine methyl ester, CAS 217178-62-6) were separated using two different procedures. The first method involved separation of the iso
- Venkatachalam, Taracad K.,Qazi, Sanjive,Uckun, Fatih M.
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p. 152 - 158
(2007/10/03)
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- 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
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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.
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p. 3121 - 3126
(2007/10/03)
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