- Zelkovamycin is an OXPHOS Inhibitory Member of the Argyrin Natural Product Family
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Natural products (NPs) are an important inspirational source for developing drugs and chemical probes. In 1999, the group of ōmura reported the constitutional elucidation of zelkovamycin. Although largely unrecognized so far, this NP displays structural s
- Krahn, Daniel,Heilmann, Geronimo,Vogel, Felix C. E.,Papadopoulos, Chrisovalantis,Zweerink, Susanne,Kaschani, Farnusch,Meyer, Hemmo,Roesch, Alexander,Kaiser, Markus
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supporting information
p. 8524 - 8531
(2020/07/02)
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- Synthesis of a novel cysteine-incorporated anthraquinone derivative and its structural properties
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A novel cysteine-incorporated anthraquinone derivative was synthesized, and its molecular structure was determined by X-ray crystal analysis. Each mercapto group was located separately and did not form a disulfide bond, and hydrogen bondings and Π-Π interaction were observed from the packing structure.
- Nomoto, Akihiro,Taniguchi, Toshihide,Minatobe, Yuta,Katao, Syouhei,Kakiuchi, Kiyomi,Yano, Shigenobu,Ogawa, Akiya
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p. 10192 - 10204
(2015/08/06)
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- Reversible crosslinking of polymers bearing pendant or terminal thiol groups prepared by nitroxide-mediated radical polymerization
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Monomers or N-alkoxyamine initiators containing protected thiol groups are utilized to prepare polymers via nitroxide-mediated radical polymerization. Following thiol deprotection, the macromolecular properties of these polymers are manipulated, by adjusting the redox conditions to either form or cleave disulfide bonds, or irreversibly cap free thiols by the rapid addition to a maleimide Michael acceptor. Formation of disulfide bonds under dilute conditions results in intramolecular disulfide formation, resulting in internal polymer collapse. Alternatively, disulfide formation under high concentration results in intermolecular crosslinking of polymers to form networked macromolecular assemblies.
- Braslau, Rebecca,Rivera III, Frank,Tansakul, Chittreeya
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p. 624 - 633
(2013/05/08)
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- AROMATIC COMPOUNDS AND METAL COMPLEXES THEREOF
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Provided are aromatic compounds and metal complexes thereof which may be useful treating various forms of proliferative diseases, such as cancer. In some instances, the metal complexes thereof are relatively stable, and may be suitable for oral administra
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Page/Page column 60
(2012/12/13)
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- An iminodiacetic acid based lanthanide binding tag for paramagnetic exchange NMR spectroscopy
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All the way with IDA! Attachment of iminodiacetic acid (IDA) to a protein helix creates a rigid lanthanide binding site that can be exploited for paramagnetic NMR spectroscopy (see picture). Pseudo-contact shifts (PCSs) larger than 8 ppm are achievable wi
- Swarbrick, James D.,Ung, Phuc,Chhabra, Sandeep,Graham, Bim
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supporting information; experimental part
p. 4403 - 4406
(2011/06/22)
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- Cyclic disulfides as functional mimics of the histone deacetylase inhibitor FK-228
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FK-228 is a potent histone deacetylase (HDAC) inhibitor with tremendous therapeutic potential against a wide array of human cancers. We describe the development of analogs that share FK-228's novel mechanism of activation and HDAC inhibition.
- Mays, Jared R.,Restituyo, José A.,Katzenberger, Rebeccah J.,Wassarman, David A.,Rajski, Scott R.
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p. 4579 - 4583
(2008/02/04)
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- seco-Cyclothialidines: New concise synthesis, inhibitory activity toward bacterial and human DNA topoisomerases, and antibacterial properties
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seco-Cyclothialidines are a promising class of bacterial DNA gyrase B subunit inhibitors. A new seco-cyclothialidine derivative containing a dioxazine moiety, BAY 50-7952, was synthesized through a new concise pathway. One key step of the synthesis is the
- Rudolph,Theis,Hanke,Endermann,Johannsen,Geschke
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p. 619 - 626
(2007/10/03)
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- Mercaptoacyl amino acid inhibitors of atriopeptidase. 1. Structure- activity relationship studies of methionine and S-alkylcysteine derivatives
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A broad series of N-(3-mercaptoacyl) amino acid derivatives was evaluated for their ability to inhibit atriopeptidase (neutral endopeptidase, EC 3.4.24.11) in vitro and in vivo. Structural parameters studied were (i) the substituent on the 2-position of the 3-mercaptopropionyl moiety, (ii) the amino acid component, (iii) the S-terminal derivative, and (iv) the C- terminal derivative. Optimum activity was observed for derivatives of methionine and S-alkylcysteines. N-[3-Mercapto-2(S)-[(2- methylphenyl)methyl]-1-oxopropyl]-L-methionine was identified as a highly effective inhibitor of atriopeptidase meriting evaluation as a potential cardiovascular therapeutic agent.
- Neustadt,Smith,Nechuta,Bronnenkant,Haslanger,Watkins,Foster,Sybertz
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p. 2461 - 2476
(2007/10/02)
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- Oxidative Deblocking of the 4-Methoxybenzyl Thioether Protecting Group: Application to the Directed Synthesis of Poly-cystinyl Peptides
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The 4-methoxybenzyl thioether protecting group is deblocked efficiently by oxidation with the homogeneous electron transfer agent tris(4-bromophenyl)ammoniumyl (2.+) leading to the disulfide in high yields.S-(4-methoxybenzyl)cysteine derivatives like 9 in this way can be transformed into the corresponding cystine derivatives like 10 in 90percent yield.Many N and carboxy protecting groups like the Boc and Z group and tert-butyl or benzyl ester functions are stable under the cleavage conditions.On the other hand the 4-methoxybenzyl thioether protecting group is totally unaffected by the conditions for oxidative deblocking of the S-trityl functions by either iodine or rhodanolysis.This opens up new opportunities for the directed synthesis of cystinyl peptides with more than one intra- or interchain disulfide bridge.Application of the new method to the synthesis of a cystine peptide with one intrachain S-S-bridge and a double-chain biscystinyl peptide is reported.
- Platen, Martin,Steckhan, Eberhard
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p. 1563 - 1576
(2007/10/02)
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