- Design, Synthesis and Evaluation of AdSS Bisubstrate Inhibitors
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Many cancers lack the expression of methylthioadenosine phosphorylase (MTAP). These cancers require adenylosuccinate synthetase (AdSS) for nucleic acid synthesis. By inhibiting adenylosuccinate synthetase, we potentially have a new therapeutic agent. Bisubstrate inhibitors were synthesized and evaluated against purified AdSS. The best activity was obtained with adenosine bearing a four-carbon linker that connects the N-formyl-N-hydroxy moiety to the 6-position of the purine nucleoside.
- Tibrewal, Nidhi,Elliott, Gregory I.
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supporting information
p. 2269 - 2272
(2020/09/17)
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- ANTIBACTERIAL SIDEROMYCINS
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A compound, comprising: an Fe(III)-binding and/or Fe(III)-bound siderophore; one or more optional linker covalently bound to the siderophore; and daptomycin covalently bound to the linker, or, if no linker is present, then to the siderophore; or pharmaceu
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Page/Page column 63
(2016/03/13)
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- The synthesis of tetrahydropyridopyrimidones as a new scaffold for HIV-1 integrase inhibitors
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An efficient synthesis of methyl 9-amino-3-hydroxy-4-oxo-6,7,8,9-tetrahydro-4H-pyrido[1,2-a]pyrimidine-2-carboxylate as a late stage intermediate for a new class of HIV-1 integrase inhibitors is described. After construction of the bicyclic core scaffold,
- Kinzel, Olaf D.,Monteagudo, Edith,Muraglia, Ester,Orvieto, Federica,Pescatore, Giovanna,Ferreira, Maria del Rosario Rico,Rowley, Michael,Summa, Vincenzo
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p. 6552 - 6555
(2008/02/12)
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- TETRAHYDRO-4H-PYRIDO[1,2-A]PYRIMIDINES AND RELATED COMPOUNDS USEFUL AS HIV INTEGRASE INHIBITORS
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Tetrahydro-4H-pyrido[1,2-a]pyrimidines and related compounds of Formula (A): are described as inhibitors of HIV integrase and inhibitors of HIV replication, wherein n is an integer equal to zero, 1, 2 or 3, and R1, R3, R4,
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- Total synthesis of the siderophore Danoxamine
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The total synthesis of the linear trihydroxamate siderophore, Danoxamine, is described. Danoxamine is a siderophore component of the naturally occurring siderophore-drug conjugates Salmycin A-D. The synthesis of Danoxamine features a series of coupling re
- Roosenberg II, John M.,Miller, Marvin J.
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p. 4833 - 4838
(2007/10/03)
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- Method for synthesis of desferrioxamine B, analogs and homologs thereof
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Synthesis of desferrioxamine B and analogs and homologs thereof beginning with O-protected, N-protected hydroxylamine, which is N-alkylated to produce a protected N-4-cyanoalkylhydroxylamine which is acylated with a suitable anhydride. The resulting half-
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- Method for the synthesis of desferrioxamine B and analogs thereof
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Disclosed is a synthesis of desferrioxamine B and analogs and homologs thereof beginning with the generation of the O-protected N-(4-cyanobutyl)hydroxylamine which is acylated at the O-benzylhydroxylamine nitrogen with either succinic or acetic anhydride. The resulting half-acid amide or amide respectively, is subjected to a series of high yield condensations and reductions which provide desferrioxamine B in 45% overall yield. Finally, a desamino analog of desferrioxamine is prepared in order to demonstrate the synthetic utility of the scheme as applied to desferrioxamine derivatives.
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- THE TOTAL SYNTHESIS OF BISUCABERIN
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The first total synthesis of 6,17-dihydroxy-1,6,12,17-tetraazacyclodocosane-2,5,13,16-tetrone (bisucaberin) is presented.The synthetic scheme employed in this study illustrates the utility of O-benzyl-N-(tert-butoxycarbonyl)-N-(4-cyanobutyl)hydroxylamine
- Bergeron, R. J.,McManis, J. S.
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p. 4939 - 4944
(2007/10/02)
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