Search Results - "Yager, Kraig"
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Structure-based design, synthesis, and study of pyrazolo[1,5-a][1,3,5]triazine derivatives as potent inhibitors of protein kinase CK2
Published in Bioorganic & medicinal chemistry letters (01-08-2007)“…Structure-guided modifications to a series of pyrazolo[1,5-a][1,3,5]triazine derivatives provided pM inhibitors of protein kinase CK2 with low μM cytotoxic…”
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Discovery of (2S)‑1-[4-(2-{6-Amino-8-[(6-bromo-1,3-benzodioxol-5-yl)sulfanyl]‑9H‑purin-9-yl}ethyl)piperidin-1-yl]-2-hydroxypropan-1-one (MPC-3100), a Purine-Based Hsp90 Inhibitor
Published in Journal of medicinal chemistry (13-09-2012)“…Modulation of Hsp90 (heat shock protein 90) function has been recognized as an attractive approach for cancer treatment, since many cancer cells depend on…”
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Novel Mps1 kinase inhibitors: From purine to pyrrolopyrimidine and quinazoline leads
Published in Bioorganic & medicinal chemistry letters (15-12-2013)“…Mps1, also known as TTK, is a mitotic checkpoint protein kinase that has become a promising new target of cancer research. In an effort to improve the…”
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Cost‐Utility of a Prognostic Test Guiding Adjuvant Chemotherapy Decisions in Early‐Stage Non‐Small Cell Lung Cancer
Published in The oncologist (Dayton, Ohio) (01-02-2016)“…Background. A prognostic test was developed to guide adjuvant chemotherapy (ACT) decisions in early‐stage non‐small cell lung cancer (NSCLC) adenocarcinomas…”
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Discovery of an l-alanine ester prodrug of the Hsp90 inhibitor, MPC-3100
Published in Bioorganic & medicinal chemistry letters (15-11-2015)“…[Display omitted] Various types of Hsp90 inhibitors have been and continue to undergo clinical investigation. One development candidate is the purine-based,…”
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Structure-Based Design, Synthesis, and Antimicrobial Activity of Indazole-Derived SAH/MTA Nucleosidase Inhibitors
Published in Journal of medicinal chemistry (18-12-2003)“…The structure-based design, synthesis, and biological activity of a novel indazole-containing inhibitor series for S-adenosyl homocysteine/methylthioadenosine…”
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Lead optimization of purine based orally bioavailable Mps1 (TTK) inhibitors
Published in Bioorganic & medicinal chemistry letters (01-07-2012)“…Efforts to optimize biological activity, novelty, selectivity and oral bioavailability of Mps1 inhibitors, from a purine based lead MPI-0479605, are described…”
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Structure-Based Design, Synthesis, and Study of Potent Inhibitors of β-Ketoacyl-acyl Carrier Protein Synthase III as Potential Antimicrobial Agents
Published in Journal of medicinal chemistry (10-03-2005)“…Fatty acid biosynthesis is essential for bacterial survival. Components of this biosynthetic pathway have been identified as attractive targets for the…”
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Enantioselective Synthesis of Diverse .alpha.-Amino Phosphonate Diesters
Published in Journal of the American Chemical Society (01-11-1995)Get full text
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Triterpene based compounds with potent anti-maturation activity against HIV-1
Published in Bioorganic & medicinal chemistry (15-12-2008)“…Efforts towards developing orally bioavailable HIV-1 maturation inhibitors starting from betulinic acid 1 are described. SAR resulted in improved potency,…”
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Peptide Synthesis Catalyzed by an Antibody Containing a Binding Site for Variable Amino Acids
Published in Science (American Association for the Advancement of Science) (08-07-1994)“…Monoclonal antibodies, induced with a phosphonate diester hapten, catalyzed the coupling of p-nitrophenyl esters of N-acetyl valine, leucine, and phenylalanine…”
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Structure-based design, synthesis, and antimicrobial activity of purine derived SAH/MTA nucleosidase inhibitors
Published in Bioorganic & medicinal chemistry letters (21-06-2004)“…Systematic, structure-guided modifications to a series of 6-substituted purine and deaza purine derivatives provided low nM inhibitors of the bacterial enzyme…”
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Investigations of an Antibody Ligase
Published in Journal of the American Chemical Society (15-01-1997)“…Further investigation of the monoclonal antibody 16G3 has revealed that it not only couples activated amino acids to form dipeptides with high turnover rates…”
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Phosphonyltriethylammonium Salts: Novel Reactive Species for the Synthesis of Phosphonate Esters and Phosphonamides
Published in Journal of the American Chemical Society (01-06-1995)Get full text
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Phosphonate Diester and Phosphonamide Synthesis. Reaction Coordinate Analysis by 31P NMR Spectroscopy: Identification of Pyrophosphonate Anhydrides and Highly Reactive Phosphonylammonium Salts1
Published in Journal of the American Chemical Society (03-09-1997)“…A series of phosphonochloridates was prepared from the corresponding phosphonate monoesters, and their reactions with alcohols, amines, and the bisnucleophile…”
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Validation of a cell cycle progression score for 5-year mortality risk in patients with stage I non-small cell lung cancer
Published in Journal of clinical oncology (20-05-2015)“…Abstract only…”
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Cell cycle progression score is a marker for five-year lung cancer-specific mortality risk in patients with resected stage I lung adenocarcinoma
Published in Oncotarget (07-06-2016)“…The goals of our study were (a) to validate a molecular expression signature (cell cycle progression [CCP] score and molecular prognostic score [mPS;…”
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