Výsledky vyhledávání - "David, Cesarz"

The Synthesis of a Novel Inhibitor of B-Raf Kinase

Autor: David Bryant Batt, Run-Ming B. Wang, Peng Geng, Markus Bänziger, Tim Ramsey, Lawrence Blas Perez, Francis Taplin, Richard William Versace, David Cesarz, Wolfgang Marterer, Walter Michael, Naeem Yusuff, Donatienne Denni-Dischert

Publikováno v: Organic Process Research & Development. 10:70-77

A scaleable synthetic route to [4,7‘]bis-isoquinolinyl-1-yl-(2-tert-butyl-pyrimidine-5-yl)amine (1), an inhibitor of B-Raf kinase is described. The key step in the synthesis is the Pd-catalyzed Negishi coupling of 4-bromo-1-chloroisoquinoline with

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::7b5919fa44d0475d8f4170643a35afec
https://doi.org/10.1021/op0501601

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N-Hydroxy-3-phenyl-2-propenamides as Novel Inhibitors of Human Histone Deacetylase with in Vivo Antitumor Activity: Discovery of (2E)-N-Hydroxy-3-[4-[[(2-hydroxyethyl)[2-(1H-indol-3-yl)ethyl]amino]methyl]phenyl]-2-propenamide (NVP-LAQ824)

Publikováno v: Journal of Medicinal Chemistry. 46:4609-4624

A series of N-hydroxy-3-phenyl-2-propenamides were prepared as novel inhibitors of human histone deacetylase (HDAC). These compounds were potent enzyme inhibitors, having IC50s < 400 nM in a partially purified enzyme assay. However, potency in cell g

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::6e0206bc14fdb324b1acbdd17eeea9cc
https://doi.org/10.1021/jm030235w

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Synthesis and Antitumor Activity of Ester-Modified Analogues of Bengamide B

Autor: John Bontempo, Jagoe Christopher Turchik, Yin Mou, Ania M. Czuchta, Penny E. Phillips, Kenneth W. Bair, Frederick Ray Kinder, Long D. Tran, Sonya Zabludoff, Steven Chen, Run-Ming Wang, David Cesarz, Raphael Nemzek, Richard William Versace, Susan Weltchek, Phillip Crews

Publikováno v: Journal of Medicinal Chemistry. 44:3692-3699

Bengamide B, a novel sponge-derived marine natural product with broad spectrum antitumor activity, was not suitable for further preclinical development because of its difficult synthesis and very poor water solubility. Bengamide B produced a 31% T/C

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::17234048bcbfe0dae8659e5596f5dcde
https://doi.org/10.1021/jm010188c

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N-hydroxy-3-phenyl-2-propenamides as novel inhibitors of human histone deacetylase with in vivo antitumor activity: discovery of (2E)-N-hydroxy-3-[4-[[(2-hydroxyethyl)[2-(1H-indol-3-yl)ethyl]amino]methyl]phenyl]-2-propenamide (NVP-LAQ824)

Publikováno v: Journal of medicinal chemistry. 46(21)

A series of N-hydroxy-3-phenyl-2-propenamides were prepared as novel inhibitors of human histone deacetylase (HDAC). These compounds were potent enzyme inhibitors, having IC(50)s400 nM in a partially purified enzyme assay. However, potency in cell gr

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::bb53e5018b4b18dfee5bd9f0a811de98
https://pubmed.ncbi.nlm.nih.gov/14521422

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Interaction of a novel GDP exchange inhibitor with the Ras protein

Publikováno v: Biochemistry. 37(45)

Mutated, tumorigenic Ras is present in a variety of human tumors. Compounds that inhibit tumorigenic Ras function may be useful in the treatment of Ras-related tumors. The interaction of a novel GDP exchange inhibitor (SCH-54292) with the Ras-GDP pro

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c8588dd08523ce1eb52765428eb0f1de
https://pubmed.ncbi.nlm.nih.gov/9843367

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