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A Parallel Approach to 7-(Hetero)arylpyrazolo[1,5-a]pyrimidin-5-ones
10.1021/acscombsci.8b00032 2018-04-06 A modular, two-pot assembly of 7-arylpyrazolo[1,5-a]pyrimidones from aryl/heteroaryl halides and aminopyrazoles in library format was developed. Sonogashira coupling of aryl bromides with triethyl orthopropiolate, followed by in situ orthoester hydrolysis, pr... |
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Solid-Phase Synthesis of β-Hydroxy Ketones Via DNA-Compatible Organocatalytic Aldol Reactions
10.1021/acscombsci.8b00001 2018-04-03 One-bead one-compound (OBOC) libraries constructed by solid-phase split-and-pool synthesis are a valuable source of protein ligands. Most OBOC libraries are composed of oligoamides, particularly peptides, peptoids, and peptoid-inspired molecules. Further dive... |
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Construction of Druglike 2-Amido Benzo[d]imidazole Analogues via Desulfurative Cyclization of Thiourea Intermediate Resin on Solid-Phase
10.1021/acscombsci.8b00004 2018-03-26 A 2-amido benzo[d]imidazole library has been constructed by solid-phase synthesis. The key step of this solid-phase synthesis involves the preparation of polymer-bound 2-amino benzo[d]imidazole resin through desulfurative cyclization of thiourea resin using 2... |
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Development and Application of a Sensitive Peptide Reporter to Discover 20S Proteasome Stimulators
10.1021/acscombsci.7b00193 2018-03-23 To attenuate an overabundance of cellular protein, it has been hypothesized that the 20S core particle (20S CP) of the proteasome can be chemically stimulated to degrade proteins into nontoxic peptides more quickly. Screening for small molecule 20S CP stimula... |
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A General Small-Angle X-ray Scattering-Based Screening Protocol Validated for Protein–RNA Interactions
10.1021/acscombsci.8b00007 2018-03-23 We present a screening protocol utilizing small-angle X-ray scattering (SAXS) to obtain structural information on biomolecular interactions independent of prior knowledge, so as to complement affinity-based screening and provide leads for further exploration.... |
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Aptamer-Based Paper Strip Sensor for Detecting Vibrio fischeri
10.1021/acscombsci.7b00190 2018-03-22 Aptamer-based paper strip sensor for detecting Vibrio fischeri was developed. Our method was based on the aptamer sandwich assay between whole live cells, V. fischeri and DNA aptamer probes. Following 9 rounds of Cell-SELEX and one of the negative-SELEX, V. f... |
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Rapid Assessment of Sputtered Nanoparticle Ionic Liquid Combinations
10.1021/acscombsci.8b00017 2018-03-21 A high-throughput method is presented for the efficient assessment of the formation and stability of nanoparticle suspensions in ionic liquids which differ in their cations and anions. As a proof of principle, Ag was sputtered on a cavity array filled with 9 ... |
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Influences of W Content on the Phase Transformation Properties and the Associated Stress Change in Thin Film Substrate Combinations Studied by Fabrication and Characterization of Thin Film V1–xWxO2 Materials Libraries
10.1021/acscombsci.7b00192 2018-03-12 The mechanical stress change of VO2 film substrate combinations during their reversible phase transformation makes them promising for applications in micro/nanoactuators. V1–xWxO2 thin film libraries were fabricated by reactive combinatorial cosputtering to i... |
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A Bioactive Trypanosoma cruzi Bromodomain Inhibitor from Chemically Engineered Extracts
10.1021/acscombsci.7b00172 2018-03-02 A set of chemically engineered extracts enriched in compounds including N–N and N–O fragments in their structures was prepared. Bromodomain binding screening and bioguided fractionation led to the identification of one oxime hit that interacts with TcBDF3 wit... |
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Comparison of Cell Permeability of Cyclic Peptoids and Linear Peptoids
10.1021/acscombsci.7b00194 2018-03-01 Cyclic peptoids are emerging as an attractive class of peptidomimetics. Compared to their linear counterparts, cyclic peptoids should have increased conformational rigidity and preorganized structures, enabling them to bind more tightly to target proteins wit... |