Search Results - "Cooper, Alan B."
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1-Thiazol-2-yl-N-3-methyl-1H-pyrozole-5-carboxylic acid derivatives as antitumor agents
Published in Bioorganic & medicinal chemistry letters (15-09-2017)“…[Display omitted] A class of substituted 1-thiazol-2-yl-N-3-methyl-1H-pyrozole-5-carboxylic acid derivatives was found to have potent anti-proliferative…”
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Discovery of 3(S)-thiomethyl pyrrolidine ERK inhibitors for oncology
Published in Bioorganic & medicinal chemistry letters (15-06-2018)“…[Display omitted] •Discovery of potent, selective and orally bioavailable ERK inhibitor for oncology.•Synthesis of tert 3-(S)thiomethyl pyrrolidine based ERK…”
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MK-8353: Discovery of an Orally Bioavailable Dual Mechanism ERK Inhibitor for Oncology
Published in ACS medicinal chemistry letters (12-07-2018)“…The emergence and evolution of new immunological cancer therapies has sparked a rapidly growing interest in discovering novel pathways to treat cancer. Toward…”
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New class of azaheptapyridine FPT inhibitors as potential cancer therapy agents
Published in Bioorganic & medicinal chemistry letters (15-02-2014)“…Tertiary hydroxyl class of C-imidazole bridgehead azaheptapyridine FPT inhibitors were prepared in an attempt to block in vivo oxidation of secondary hydroxyl…”
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Pyrazolo[1,5- a]pyrimidine-based inhibitors of HCV polymerase
Published in Bioorganic & medicinal chemistry letters (15-11-2009)“…Synthesis and optimization of novel pyrazolo[1,5- a]pyrimidine HCV polymerase inhibitors are described. The present paper describes a novel series of HCV RNA…”
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Discovery of 4H-pyrazolo[1,5-a]pyrimidin-7-ones as potent inhibitors of hepatitis C virus polymerase
Published in Bioorganic & medicinal chemistry letters (15-09-2009)“…A series of 4H-pyrazolo[1,5-a]pyrimidin-7-one derivatives was synthesized and evaluated for inhibitory activity against HCV NS5B RNA-dependent RNA polymerase…”
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Discovery of C-imidazole azaheptapyridine FPT inhibitors
Published in Bioorganic & medicinal chemistry letters (01-02-2010)“…The discovery of C-linked imidazole azaheptapyridine bridgehead FPT inhibitors is described. This novel class of compounds are sub nM FPT enzyme inhibitors…”
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Total synthesis of the antifungal cyclic depsipeptides Sch 57697 and aureobasidin A
Published in Tetrahedron letters (05-08-1996)“…A novel cyclic depsinonapeptide antifungal 1a (Sch 57697) and its isomer 1b were synthesized by a fragment coupling approach and this methodology was applied…”
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(+)-4-[2-[4-(8-Chloro-3,10-dibromo-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]- pyridin-11(R)-yl)-1-piperidinyl]-2-oxo-ethyl]-1-piperidinecarboxamide (SCH-66336): A Very Potent Farnesyl Protein Transferase Inhibitor as a Novel Antitumor Agent
Published in Journal of medicinal chemistry (19-11-1998)“…We have previously shown that appropriate modification of the benzocycloheptapyridine tricyclic ring system can provide potent farnesyl protein transferase…”
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Guiding farnesyltransferase inhibitors from an ECLiPS ® library to the catalytic zinc
Published in Bioorganic & medicinal chemistry letters (01-02-2006)“…Compounds 8 and 41 are potent analogs of farnesyltransferase inhibitors that were identified from an ECLiPS ® library screen. X-ray crystallographic analyses…”
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Aminothiazole inhibitors of HCV RNA polymerase
Published in Bioorganic & medicinal chemistry letters (03-01-2005)“…[Display omitted] Aminothiazole-based inhibitors designed for HCV polymerase display low micromolar potencies in biochemical assays. These compounds show a…”
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Transcription of Fragments of Lectures in 1948 by Harry Stack Sullivan
Published in Psychiatry (Washington, D.C.) (2006)“…Psychiatrist Harry Stack Sullivan, like virtually all psychiatrists of his era, was originally exposed to classic psychoanalytic theory and underwent some 200…”
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Synthesis of 5,6-dihydro-11H-benzo[5,6]-cyclohepta[1,2-b]pyridin-11-ylidene)-1-piperidine-N-cyanoguanidine derivatives as inhibitors of ras farnesyl protein transferase
Published in Bioorganic & medicinal chemistry letters (25-02-2002)“…A series of novel N-cyanoguanidine tricyclic farnesyl protein transferase (FPT) inhibitors was prepared. Replacement of a piperidine amide-group with a…”
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Structure-based drug design of clinical compound MK-8353, a novel inhibitor of ERK
Published in Acta crystallographica. Section A, Foundations and advances (20-07-2018)“…Abstract only…”
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[3+2] Cycloaddition-mediated synthesis of 3-methylsulfanyl-pyrrolidine-3-carboxylic acid methyl ester
Published in Tetrahedron letters (23-09-2009)“…Montmorollonite K-10 was found to be an efficient catalyst for the [3+2] annulation of thiomethylacrylate 2 and azomethine ylide precursor 3 towards the…”
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Discovery of 4 H-pyrazolo[1,5- a]pyrimidin-7-ones as potent inhibitors of hepatitis C virus polymerase
Published in Bioorganic & medicinal chemistry letters (2009)“…The design, synthesis and evaluation of a series of 4 H-Pyrazolo[1,5- a]pyrimidin-7-ones as potent inhibitors of hepatitis C virus polymerase are described. A…”
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Transcription of fragments of lectures in 1948 by Harry Stack Sullivan. Commentary
Published in Psychiatry (Washington, D.C.) (2006)Get full text
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Synthesis of 5,6-Dihydro-11 H-benzo[5,6]-cyclohepta[1,2- b]pyridin-11-ylidene)-1-piperidine- N-cyanoguanidine Derivatives as Inhibitors of Ras Farnesyl Protein Transferase
Published in Bioorganic & medicinal chemistry letters (2002)“…A series of novel N-cyanoguanidine tricyclic farnesyl protein transferase (FPT) inhibitors was prepared. Replacement of a piperidine amide-group with a…”
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