Search Results - "Yen‐Pon, Expédite"
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Strain‐Promoted 1,3‐Dithiolium‐4‐olates–Alkyne Cycloaddition
Published in Angewandte Chemie International Edition (07-10-2019)“…Reported here is the reactivity of mesoionic 1,3‐dithiolium‐4‐olates towards strained alkynes, leading to thiophene cycloaddition products. In the process, the…”
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Strain‐Promoted 1,3‐Dithiolium‐4‐olates–Alkyne Cycloaddition
Published in Angewandte Chemie (07-10-2019)“…Reported here is the reactivity of mesoionic 1,3‐dithiolium‐4‐olates towards strained alkynes, leading to thiophene cycloaddition products. In the process, the…”
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3
On-DNA Hydroalkylation to Introduce Diverse Bicyclo[1.1.1]pentanes and Abundant Alkyls via Halogen Atom Transfer
Published in Journal of the American Chemical Society (13-07-2022)“…DNA-encoded libraries have proven their tremendous value in the identification of new lead compounds for drug discovery. To access libraries in new chemical…”
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4
Sydnone-Based Approach to Heterohelicenes through 1,3-Dipolar-Cycloadditions
Published in Journal of the American Chemical Society (30-01-2019)“…The first approach to pyrazole-containing helicenes via sydnone-aryne [3 + 2]-cycloaddition is described. An unprecedented regioselectivity in the…”
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5
Exploiting the sp2 character of bicyclo[1.1.1]pentyl radicals in the transition-metal-free multi-component difunctionalization of [1.1.1]propellane
Published in Nature chemistry (21-07-2022)“…Strained bicyclic substructures are increasingly relevant in medicinal chemistry discovery research because of their role as bioisosteres. Over the last…”
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Design, Synthesis, and Biological Evaluation of Covalent Inhibitors of Focal Adhesion Kinase (FAK) against Human Malignant Glioblastoma
Published in Journal of medicinal chemistry (12-11-2020)“…Human malignant glioblastoma (GBM) is a highly invasive and lethal brain tumor. Targeting of integrin downstream signaling mediators in GBM such as focal…”
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Reversing Reactivity: Stereoselective Desulfurative 1,2-trans-O‑Glycosylation of Anomeric Thiosugars with Carboxylic Acids under Copper or Cobalt Catalysis
Published in Journal of organic chemistry (17-07-2020)“…We have discovered a new mode of reactivity of 1-thiosugars in the presence of Cu(II) or Co(II) for a stereoselective O-glycosylation reaction. The process…”
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Heterohelicenes through 1,3-Dipolar Cycloaddition of Sydnones with Arynes: Synthesis, Origins of Selectivity, and Application to pH-Triggered Chiroptical Switch with CPL Sign Reversal
Published in JACS Au (28-06-2021)“…Regioselective access to heterohelicenes through the 1,3-dipolar cycloaddition of sydnones with arynes is described. Novel access to sydnones and…”
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Convergent Strategy to Dizocilpine MK-801 and Derivatives
Published in Journal of organic chemistry (06-04-2018)“…A convergent total synthesis of MK-801 has been achieved. Key synthetic transformations include a multicomponent Barbier-type reaction to construct the…”
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Design, Synthesis, and Evaluation of Novel Imidazo[1,2‑a][1,3,5]triazines and Their Derivatives as Focal Adhesion Kinase Inhibitors with Antitumor Activity
Published in Journal of medicinal chemistry (08-01-2015)“…A series of triazinic inhibitors of focal adhesion kinase (FAK) have been recently shown to exert antiangiogenic activity against HUVEC cells and anticancer…”
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Structure-Based Design, Synthesis, and Characterization of the First Irreversible Inhibitor of Focal Adhesion Kinase
Published in ACS chemical biology (17-08-2018)“…Focal Adhesion Kinase signaling pathway and its functions have been involved in the development and aggressiveness of tumor malignancy, it then presents a…”
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12
Fluorogenic probes based on polycyclic sydnone scaffolds
Published in Tetrahedron (18-12-2020)“…We report the synthesis, photophysical characterization and kinetics of a series of polycyclic sydnone derivatives as a potential new class of fluorogenic…”
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13
Microwave-assisted synthesis of 2,5-disubstituted pyrimidine derivatives via Buchwald-Hartwig amination
Published in Tetrahedron letters (16-01-2020)“…[Display omitted] •A practical procedure was developed to prepare 2,5-disubstituted pyrimidines.•The method has a wide range of substrate scope and good…”
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14
Padlocking dihydrofurannulation for the control of small degree of helicity built on a fused-tetracyclic core
Published in Chemical science (Cambridge) (15-05-2024)“…Enantioselective construction of small molecules displaying a configurationally stable helical shape built on a fused-tetracyclic core is a daunting synthetic…”
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15
Synthesis of aryl-thioglycopeptides through chemoselective Pd-mediated conjugation
Published in Chemical science (Cambridge) (14-12-2018)“…We describe herein a Pd-catalyzed methodology for the thioglycoconjugation of iodoaryl peptides and aminoacids. This operationally simple process occurs under…”
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Correction: Padlocking dihydrofurannulation for the control of small degree of helicity built on a fused-tetracyclic core
Published in Chemical science (Cambridge) (25-09-2024)“…[This corrects the article DOI: 10.1039/D4SC00745J.]…”
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Sydnone-Based Approach to Heterohelicenes through 1,3-Dipolar-Cycloadditions
Published in Journal of the American Chemical Society (10-01-2019)Get full text
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18
Sydnone-based Approach to Hetero-helicenes Through 1,3-Dipolar-Cycloadditions
Published in Journal of the American Chemical Society (10-01-2019)“…The first approach to pyrazole containing helicenes via sydnone-aryne [3+2]-cycloaddition is described. An unprecedented regioselectivity in the cycloaddition…”
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19
Exploiting the sp 2 character of bicyclo[1.1.1]pentyl radicals in the transition-metal-free multi-component difunctionalization of [1.1.1]propellane
Published in Nature chemistry (01-09-2022)“…Strained bicyclic substructures are increasingly relevant in medicinal chemistry discovery research because of their role as bioisosteres. Over the last…”
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20
Synthesis of aryl-thioglycopeptides through chemoselective Pd-mediated conjugationElectronic supplementary information (ESI) available: General, experimental procedures, and characterization of all new compounds. See DOI: 10.1039/c8sc02370k
Published 28-11-2018“…We describe herein a Pd-catalyzed methodology for the thioglycoconjugation of iodoaryl peptides and aminoacids. This operationally simple process occurs under…”
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