Zobrazeno 1 - 10 of 10 pro vyhledávání: '"Jerome C Bressi"'
1
Exploration of the HDAC2 foot pocket: Synthesis and SAR of substituted N-(2-aminophenyl)benzamides
Autor: Ron de Jong, Shawn M. O’Connell, Robert Melkus, Andrew John Jennings, Marc Navre, Jerome C. Bressi, Anthony R. Gangloff, Yiqin Wu, Charles E. Grimshaw, Robert J. Skene
Publikováno v: Bioorganic & Medicinal Chemistry Letters. 20:3142-3145
A series of N-(2-amino-5-substituted phenyl)benzamides (3-21) were designed, synthesized and evaluated for their inhibition of HDAC2 and their cytotoxicity in HCT116 cancer cells. Multiple compounds from this series demonstrated time-dependent bindin
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::acc77bb996c8a35bb0284c71c769c99d
https://doi.org/10.1016/j.bmcl.2010.03.091
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2
A new prodrug of paclitaxel: synthesis of Protaxel
Autor: Milos Sovak, Jerome C Bressi, James Gordon Douglass, Allen L. Seligson, Terry Ronald C
Publikováno v: Anti-Cancer Drugs. 12:305-313
2' and 7 Polyol carbonates of paclitaxel were synthesized and screened as potential paclitaxel prodrugs. Paclitaxel is released from 7-(2",3"-dihydroxypropylcarbonato) paclitaxel (Protaxel) at rates inversely proportional to pH, by an intramolecular
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fa35300920f67ea99672a2552eba1a64
https://doi.org/10.1097/00001813-200104000-00002
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3
A disubstituted NAD + analogue is a nanomolar inhibitor of trypanosomal glyceraldehyde-3-phosphate dehydrogenase
Autor: Jerome C. Bressi, Kevin J Kennedy, Michael H. Gelb
Publikováno v: Bioorganic & Medicinal Chemistry Letters. 11:95-98
N6-Naphthalenemethyl-2'-methoxybenzamido-beta-NAD+, a derivative of a low micromolar first-generation inhibitor of trypanosomal glyceraldehyde phosphate dehydrogenase (GAPDH), was synthesized, taking advantage of methodology for the selective phosphi
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::043e3b31c96e3b2bc8f4565c3059bee6
https://doi.org/10.1016/s0960-894x(00)00608-9
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4
Adenosine Analogues as Inhibitors of Trypanosoma brucei Phosphoglycerate Kinase: Elucidation of a Novel Binding Mode for a 2-Amino-N6-Substituted Adenosine
Autor: Wim G. J. Hol, Christophe L. M. J. Verlinde, Michael H. Gelb, Jungwoo Choe, Wesley C. Van Voorhis, Melinda T. Hough, Jerome C. Bressi, Frederick S. Buckner
Publikováno v: Journal of Medicinal Chemistry. 43:4135-4150
As part of a project aimed at structure-based design of adenosine analogues as drugs against African trypanosomiasis, N(6)-, 2-amino-N(6)-, and N(2)-substituted adenosine analogues were synthesized and tested to establish structure-activity relations
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9052aa282098f22de4df1952c83ccbaa
https://doi.org/10.1021/jm000287a
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5
Benzimidazole and imidazole inhibitors of histone deacetylases: Synthesis and biological activity
Autor: Leslie W. Tari, Phong H. Vu, Anthony R. Gangloff, Marc Navre, Yiqin Wu, Jerome C. Bressi, Robert J. Skene, Ron de Jong, Jason W. Brown, Xiaodong Cao, Andrew John Jennings, Shawn M. O’Connell
Publikováno v: Bioorganicmedicinal chemistry letters. 20(10)
A series of N-hydroxy-3-[3-(1-substituted-1H-benzoimidazol-2-yl)-phenyl]-acrylamides (5a–5ab) and N-hydroxy-3-[3-(1,4,5-trisubstituted-1H-imidazol-2-yl)-phenyl]-acrylamides (12a–s) were designed, synthesized, and found to be nanomolar inhibitors
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::eec06bf3fd4f1858b761d04380c60353
https://pubmed.ncbi.nlm.nih.gov/20392637
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7
Conformational changes in Leishmania mexicana glyceraldehyde-3-phosphate dehydrogenase induced by designed inhibitors
Autor: Christophe L. M. J. Verlinde, Kevin J Kennedy, Wim G. J. Hol, Jerome C. Bressi, Michael H. Gelb, Stephen Suresh
Publikováno v: Journal of molecular biology. 309(2)
The glycolytic enzymes of trypanosomes are attractive drug targets, since the blood-stream form of Trypanosoma brucei lacks a functional citric acid cycle and is dependent solely on glycolysis for its energy requirements. Glyceraldehyde-3-phosphate d
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0f2b54b905a79d59b6f7ae1f708cad4f
https://pubmed.ncbi.nlm.nih.gov/11371162
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8
Polymer-assisted solution-phase synthesis of 2'-amido-2'-deoxyadenosine derivatives targeted at the NAD(+)-binding sites of parasite enzymes
Autor: Abolfasl Golisade, Jerome C. Bressi, Andreas Link, Michael H. Gelb, Serge Van Calenbergh
Publikováno v: Journal of combinatorial chemistry. 2(5)
A polymer-assisted solution-phase (PASP) synthesis of lead structure analogues ready for biological testing without the demand for chromatographic purification is described. Carboxylic acids are coupled to the Kenner or Ellman safety catch linker, re
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a247d854c0b7fa06f1cd1d8d34ef8ce5
https://pubmed.ncbi.nlm.nih.gov/11029179
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9
A bisubstrate analog induces unexpected conformational changes in phosphoglycerate kinase from Trypanosoma brucei
Autor: David M. Williams, G.M. Blackburn, Peter Kuhn, Wim G. J. Hol, Jerome C. Bressi, Michael H. Gelb, Bradley E. Bernstein
Publikováno v: Journal of molecular biology. 279(5)
The glycolytic enzyme phosphoglycerate kinase (PGK) catalyzes phosphoryl transfer between 1,3-bis-phosphoglycerate and ADP to form 3-phosphoglycerate and ATP. During catalysis, a major hinge bending motion occurs which brings the N and C-terminal enz
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7e3a2a2def54fc9e768acab6cf235447
https://pubmed.ncbi.nlm.nih.gov/9642090
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10
Protein structure-based design of anti-protozoal drugs
Autor: Frederick S. Buckner, Wesley C. Van Voorhis, Wim G. J. Hol, Stephen Suresh, Christophe L. M. J. Verlinde, Jungwoo Choe, Jerome C. Bressi, Michael H. Gelb, Paul A.M. Michels
Publikováno v: Journal of the Brazilian Chemical Society, Vol 13, Iss 6, Pp 843-844 (2002)
Journal of the Brazilian Chemical Society, Volume: 13, Issue: 6, Pages: 843-844, Published: NOV 2002
Journal of the Brazilian Chemical Society v.13 n.6 2002
Journal of the Brazilian Chemical Society
Sociedade Brasileira de Química (SBQ)
instacron:SBQ
The repertory of drugs to fight protozoal diseases such as malaria, Chagas' disease, leishmaniasis, and African trypanosomiasis is woefully inadequate. Now, genome sequencing and structural genomics projects are quickly elucidating new drug targets,
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2411fdc4e74f5ee6cd26a00d2a940e9c
http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0103-50532002000600018
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