John E. Toth

Cdk1 Activity Is Required for Mitotic Activation of Aurora A during G2/M Transition of Human Cells

Robert D. Van Horn, Shaoyou Chu, Fan Li, Tinggui Yin et autres

In mammalian cells entry into and progression through mitosis are regulated by multiple mitotic kinases. How mitotic kinases interact with each other and coordinately regulate mitosis remains to be fully understood. Here we employed a chemical biology approach using selective small molecule …

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ChemInform Abstract: A Concise Synthesis of Quinazolinone TGF‐β RI Inhibitor Through One‐Pot Three‐Component Suzuki—Miyaura/Etherification and Imidate—Amide Rearrangement Reactions.

Hongyu Li, Yan Wang, William T. McMillen, Arindam Chatterjee et autres

Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article …

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Imidazolyl benzimidazoles and imidazo[4,5-b]pyridines as potent p38α MAP kinase inhibitors with excellent in vivo antiinflammatory properties

Mary M. Mader, Alfonso de Dios, Chuan Shih, Rosanne Bonjouklian et autres

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A concise synthesis of quinazolinone TGF-β RI inhibitor through one-pot three-component Suzuki–Miyaura/etherification and imidate–amide rearrangement reactions

Hongyu Li, Yan Wang, William T. McMillen, Arindam Chatterjee et autres

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Mitotic requirement for aurora A kinase is bypassed in the absence of aurora B kinase

Hui Yang, Teresa F. Burke, Jack Dempsey, Bruce Diaz et autres

We investigated why treatment of cells with dual aurora A and B kinase inhibitors produces phenotypes identical to inactivation of aurora B. We found that dual aurora kinase inhibitors in fact potently inhibit cellular activities of both kinases, indicating that inactivation of …

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Complete Inhibition of Anisomycin and UV Radiation but Not Cytokine Induced JNK and p38 Activation by an Aryl-substituted Dihydropyrrolopyrazole Quinoline and Mixed Lineage Kinase 7 Small Interfering RNA

Xushan Wang, Mary M. Mader, John E. Toth, Xiaohong Yu et autres

Mixed lineage kinase 7 (MLK7) is a mitogen-activated protein kinase kinase kinase (MAPKKK) that activates the pro-apoptotic signaling pathways p38 and JNK. A library of potential kinase inhibitors was screened, and a series of dihydropyrrolopyrazole quinolines was identified as highly potent inhibitors …

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p-Toluenesulfonyl Bromide

John E. Toth, Elizabeth Collins

[1950-69-2] C7H7BrO2S (MW 235.10) InChI = 1S/C7H7BrO2S/c1-6-2-4-7(5-3-6)11(8,9)10/h2-5H,1H3 InChIKey = NTSFJZORNYYLFW-UHFFFAOYSA-N (reagent used as a radical cyclization initiator and sulfonating, halogenating reagent) Alternate Name: 4-methylbenzenesulfonyl bromide, tosyl bromide, TsBr. Physical Data: mp 95–96 °C. Solubility: sparingly soluble in H2O; soluble in toluene, benzene, …

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Synthesis and in vitro Antimicrobial Activity of 3‐Keto 16‐Membered Macrolides Derived from Tylosin.

Lawrence C. Creemer, John E. Toth, Herbert A. Kirst

Abstract For Abstract see ChemInform Abstract in Full Text.

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ChemInform Abstract: Synthesis and Structure—Activity Relationship Studies of Cryptophycins: A Novel Class of Potent Antimitotic Antitumor Depsipeptides

Chuan Shih, Rima Al‐awar, Andrew H. Fray, Michael J. Martinelli et autres

Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article …

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Synthesis and In Vitro Antimicrobial Activity of 3-Keto 16-Membered Macrolides Derived From Tylosin.

Lawrence C. Creemer, John E. Toth, Herbert A. Kirst

Several series of 14-membered ketolides derived from erythromycin exhibit useful antimicrobial activity against macrolide-resistant bacteria. To determine if 16-membered ketolides may possess analogous activity, 3-keto derivatives of 5-O-mycaminosyl-23-O-acetyltylonolide and desmycosin were synthesized by protection of susceptible functional groups, oxidation of the 3-hydroxyl …

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Synthesis and Structure-Activity Relationship Studies of Cryptophycins: A Novel Class of Potent Antimitotic Antitumor Depsipeptides

Chuan Shih, Rima Al‐awar, Andrew H. Fray, Michael J. Martinelli et autres

Detailed structure-activity relationship studies of the cryptophycin series of compounds are described. From these extensive SAR efforts, cryptophycin 52 (LY355703) was selected as the first generation cryptophycin for clinical development. The chemical synthesis and pharmacological evaluation of LY355703 and its corresponding chlorohydrin …

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Structures of Three Inhibitor Complexes Provide Insight into the Reaction Mechanism of the Human Methylenetetrahydrofolate Dehydrogenase/Cyclohydrolase

Andrea Schmidt, Haiping Wu, Robert E. MacKenzie, Victor J. Chen et autres

Enzymes involved in tetrahydrofolate metabolism are of particular pharmaceutical interest, as their function is crucial for amino acid and DNA biosynthesis. The crystal structure of the human cytosolic methylenetetrahydrofolate dehydrogenase/cyclohydrolase (DC301) domain of a trifunctional enzyme has been determined previously with a …

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