Search Results - "Aversa, Robert J"
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Continuing Saga of the Marine Polyether Biotoxins
Published in Angewandte Chemie (International ed.) (01-01-2008)“…The unprecedented structure of the marine natural product brevetoxin B was elucidated by the research group of Nakanishi and Clardy in 1981. The ladderlike…”
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Synthesis of the ABCDEFG Ring System of Maitotoxin
Published in Journal of the American Chemical Society (19-05-2010)“…Maitotoxin (1) continues to fascinate scientists not only because of its size and potent neurotoxicity but also due to its molecular architecture. To provide…”
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3
Synthesis of the C′D′E′F′ Domain of Maitotoxin
Published in Journal of the American Chemical Society (19-01-2011)“…A devised biomimetic strategy toward the C′D′E′F′ domain (6) of maitotoxin (1) led to hydroxy triepoxide 8 as a postulated polyepoxide precursor. However, all…”
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4
Chemical Synthesis of the GHIJK Ring System and Further Experimental Support for the Originally Assigned Structure of Maitotoxin
Published in Angewandte Chemie (International ed.) (01-01-2007)“…Accepting the proposal: The originally proposed structure of maitotoxin has recently come under scrutiny based on biosynthetic and computational…”
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Chemical Synthesis of the GHIJKLMNO Ring System of Maitotoxin
Published in Journal of the American Chemical Society (11-06-2008)“…As the largest secondary metabolite to be discovered as of yet, the polyether marine neurotoxin maitotoxin constitutes a major structural and synthetic…”
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Structure-Based Drug Design of Novel Potent and Selective Tetrahydropyrazolo[1,5‑a]pyrazines as ATR Inhibitors
Published in ACS medicinal chemistry letters (08-01-2015)“…A saturation strategy focused on improving the selectivity and physicochemical properties of ATR inhibitor HTS hit 1 led to a novel series of highly potent and…”
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7
Maitotoxin: An Inspiration for Synthesis
Published in Israel journal of chemistry (01-04-2011)“…Maitotoxin holds a special place in the annals of natural products chemistry as the largest and most toxic secondary metabolite known to date. Its fascinating,…”
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Design and Discovery of N‑(3-(2-(2-Hydroxyethoxy)-6-morpholinopyridin-4-yl)-4-methylphenyl)-2-(trifluoromethyl)isonicotinamide, a Selective, Efficacious, and Well-Tolerated RAF Inhibitor Targeting RAS Mutant Cancers: The Path to the Clinic
Published in Journal of medicinal chemistry (12-03-2020)“…Direct pharmacological inhibition of RAS has remained elusive, and efforts to target CRAF have been challenging due to the complex nature of RAF signaling,…”
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Design and Discovery of N‑(2-Methyl-5′-morpholino-6′-((tetrahydro‑2H‑pyran-4-yl)oxy)-[3,3′-bipyridin]-5-yl)-3-(trifluoromethyl)benzamide (RAF709): A Potent, Selective, and Efficacious RAF Inhibitor Targeting RAS Mutant Cancers
Published in Journal of medicinal chemistry (22-06-2017)“…RAS oncogenes have been implicated in >30% of human cancers, all representing high unmet medical need. The exquisite dependency on CRAF kinase in KRAS mutant…”
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10
Synthesis of the C'D'E'F' domain of maitotoxin
Published in Journal of the American Chemical Society (19-01-2011)“…A devised biomimetic strategy toward the C'D'E'F' domain (6) of maitotoxin (1) led to hydroxy triepoxide 8 as a postulated polyepoxide precursor. However, all…”
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11
Structure-Based Drug Design of Novel, Potent, and Selective Azabenzimidazoles (ABI) as ATR Inhibitors
Published in ACS medicinal chemistry letters (08-01-2015)“…Compound 13 was discovered through morphing of the ATR biochemical HTS hit 1. The ABI series was potent and selective for ATR. Incorporation of a 6-azaindole…”
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12
Cover Picture: Maitotoxin: An Inspiration for Synthesis (Isr. J. Chem. 3-4/2011)
Published in Israel journal of chemistry (01-04-2011)Get full text
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13
Chemical Synthesis of the GHIJK Ring System and Further Experimental Support for the Originally Assigned Structure of Maitotoxin
Published in Angewandte Chemie (26-11-2007)“…Bestätigung für einen Vorschlag: Die ursprünglich vorgeschlagene Struktur von Maitotoxin wurde kürzlich durch Erwägungen zur Biosynthese und Rechnungen infrage…”
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Cover Picture: The Continuing Saga of the Marine Polyether Biotoxins (Angew. Chem. Int. Ed. 38/2008)
Published in Angewandte Chemie International Edition (08-09-2008)“…An odyssey is described by K. C. Nicolaou et al. in their Review on page 7182 ff.: From the isolation of the first marine biotoxin with a ladder structure,…”
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Titelbild: Die Entdeckung und Synthese von marinen Polyethern (Angew. Chem. 38/2008)
Published in Angewandte Chemie (08-09-2008)“…Eine Odyssee erzählen K. C. Nicolaou et al. in ihrem Aufsatz auf S. 7292 ff. nach: Von der Isolierung von Brevetoxin B, dem ersten marinen Biotoxin mit…”
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Die Entdeckung und Synthese von marinen Polyethern
Published in Angewandte Chemie (08-09-2008)“…Die beispiellose Struktur des marinen Naturstoffs Brevetoxin B wurde 1981 von den Arbeitsgruppen um Nakanishi und Clardy aufgeklärt. Das leiterförmige…”
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Titelbild: Die Entdeckung und Synthese von marinen Polyethern (Angew. Chem. 38/2008)
Published in Angewandte Chemie (08-09-2008)Get full text
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