- PROCESS FOR THE PREPARATION OF A SULFUR-AMINE
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The present invention relates to a process for the synthesis of cysteamine or a salt thereof.
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- Constrained (l-)-S-adenosyl-l-homocysteine (SAH) analogues as DNA methyltransferase inhibitors
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Potent SAH analogues with constrained homocysteine units have been designed and synthesized as inhibitors of human DNMT enzymes. The five membered (2S,4S)-4-mercaptopyrrolidine-2-carboxylic acid, in 1a, was a good replacement for homocysteine, while the corresponding six-member counterpart was less active. Further optimization of 1a, changed the selectivity profile of these inhibitors. A Chloro substituent at the 2-position of 1a, compound 1d, retained potency against DNMT1, while N6 alkylation, compound 7a, conserved DNMT3b2 activity. The concomitant substitutions of 1a at both 2- and N6 positions reduced activity against both enzymes.
- Isakovic, Ljubomir,Saavedra, Oscar M.,Llewellyn, David B.,Claridge, Stephen,Zhan, Lijie,Bernstein, Naomy,Vaisburg, Arkadii,Elowe, Nadine,Petschner, Andrea J.,Rahil, Jubrail,Beaulieu, Norman,Gauthier, France,MacLeod, A. Robert,Delorme, Daniel,Besterman, Jeffrey M.,Wahhab, Amal
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scheme or table
p. 2742 - 2746
(2010/03/03)
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- Synthesis and evaluation of chloromethyl sulfoxides as a new class of selective irreversible cysteine protease inhibitors
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The synthesis and biological evaluation of a new class of selective irreversible cysteine protease inhibitors is described. A set of amino acid based chloromethyl sulfoxides was prepared and they were found to inhibit irreversibly the cysteine protease papain. They were selective for cysteine proteases since no inhibition was found for the serine protease chymotrypsin.
- Brouwer, Arwin J.,Bunschoten, Anton,Liskamp, Rob M.J.
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p. 6985 - 6993
(2008/03/28)
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- Synthesis of conjugated diacetylene, metal-chelating monomers for polymerizable monolayer assemblies.
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[see structure]. Self-assembled monolayers (SAMs) of thiols on gold have been used for numerous applications. For protein targeting applications, one successful strategy is to use a metal-chelating SAM. It has also been demonstrated that polymerized SAMs
- Roy,Mallik
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p. 1877 - 1879
(2007/10/03)
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- Synthesis of Azocine Derivatives from Thioaldehyde Diels-Alder Adducts
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Nitrogen-containing phenacyl sulfides 1 or 2 can be readily cleaved to thioaldehydes that are trapped by electron-rich dienes to give the adducts 4, 5, 11, or 17.The adducts have electrophilic character α to sulfur and can be converted into structures having new C-N bonds at the α-carbon.Thus, 4 leads to lactam 6 by S to N acyl transfer.A similar reaction occurs from 15 to the eight-membered 16.Internal addition of amine nitrogen to Danishefsky diene adducts 11, 17, or 26 affords bicyclic aminals which are converted into azocine derivatives upon desulfurization.Stable structures such as 24, 25, and 31 are prepared in this way.The unusual enaminone 20 is not stable and rearranges upon attempted purification to 21.
- Vedejs, E.,Stults, J. S.
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p. 2226 - 2232
(2007/10/02)
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