- First synthesis of novel aminophenyl pyridinium-5-(hydroxybenzoyl)-hydrazonomethyl-2-oxothiazol-3-ide derivatives and evaluation of their anticancer activities
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The first total synthesis for large-scale production and anticancer activity of novel aminophenylpyridinium-5-(hydroxybenzoyl)hydrazonomethyl-2-oxothiazol-3-ide (PBHT) (1) and its derivatives are reported. The chemical structure of PBHT was unambiguously
- Min, Dongguk,Han, Moon Hi,Lee, Seulki,Jung, Mankil
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p. 843 - 847
(2015/11/27)
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- Discovery of ANA975: An oral prodrug of the TLR-7 agonist isatoribine
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ANA975, a 5-amino-3-β-D-ribofuranosyl-3H-thiazolo[4,5-d]pyrimidin-2- one derivative, was synthesized in the search of an oral prodrug of isatoribine, a small molecule toll-like receptor 7 (TLR-7) agonist. Several strategies were studied to enable the kilogram-scale synthesis of ANA975. Three general total syntheses are described. In the phase I clinical study of ANA975 against hepatitis C virus (HCV), conversion to isatoribine in plasma was rapid and effective, delivering levels of isatoribine that have been shown to be clinically relevant. Copyright Taylor & Francis Group, LLC.
- Xiang, Alan X.,Webber, Stephen E.,Kerr, Bradley M.,Rueden, Erik J.,Lennox, Joseph R.,Haley, Gregory J.,Wang, Tingmin,Ng, John S.,Herbert, Mark R.,Clark, David L.,Banh, Virginia N.,Li, Wei,Fletcher, Simon P.,Steffy, Kevin R.,Bartkowski, Darian M.,Kirkovsky, Leonid I.,Bauman, Lisa A.,Averett, Devron R.
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p. 635 - 640
(2008/09/16)
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- 3-β-D-RIBOFURANOSYLTHIAZOLO[4,5-d]PYRIDIMINE NUCLEOSIDES AND USES THEREOF
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The invention is directed to 3-?-D-ribofuranosylthiazolo[4,5-d]pyridimine nucleosides and pharmaceutical compositions containing such compounds that have immunomodulatory activity. The invention is also directed to the therapeutic or prophylactic use of such compounds and compositions, and to methods of treating diseases and disorders described herein, by administering effective amounts of such compounds.
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Page/Page column 91; 92
(2010/02/15)
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