Search Results - "Taoda, Yoshiyuki"
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Epigenetic Regulation of Autophagy by the Methyltransferase G9a
Published in Molecular and Cellular Biology (01-10-2013)“…Article Usage Stats Services MCB Citing Articles Google Scholar PubMed Related Content Social Bookmarking CiteULike Delicious Digg Facebook Google+ Mendeley…”
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Boron Cluster-based Development of Potent Nonsecosteroidal Vitamin D Receptor Ligands: Direct Observation of Hydrophobic Interaction between Protein Surface and Carborane
Published in Journal of the American Chemical Society (28-12-2011)“…We report here the design and synthesis of a novel vitamin D receptor (VDR) agonist whose hydrophobic core structure is p-carborane…”
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Practical and Scalable Synthetic Method for Preparation of Dolutegravir Sodium: Improvement of a Synthetic Route for Large-Scale Synthesis
Published in Organic process research & development (19-04-2019)“…A practical and scalable synthetic method to obtain dolutegravir sodium (1) was established starting from the readily accessible material maltol (2). This…”
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Carbamoyl Pyridone HIV‑1 Integrase Inhibitors. 1. Molecular Design and Establishment of an Advanced Two-Metal Binding Pharmacophore
Published in Journal of medicinal chemistry (25-10-2012)“…Our group has focused on expanding the scope of a two-metal binding pharmacophore concept to explore HIV-1 integrase inhibitors through medicinal chemistry…”
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Synthesis and structure–activity relationship of p-carborane-based non-secosteroidal vitamin D analogs
Published in Bioorganic & medicinal chemistry (15-02-2014)“…1α,25-Dihydroxyvitamin D3 [1α,25(OH)2D3: 1] is a specific modulator of nuclear vitamin D receptor (VDR), and novel vitamin D analogs are therapeutic candidates…”
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New designs for HIV-1 integrase inhibitors: a patent review (2018-present)
Published in Expert opinion on therapeutic patents (02-01-2023)“…Combination antiretroviral therapy (cART) has dramatically reduced morbidity and mortality of HIV-1-infected patients. Integrase strand transfer inhibitors…”
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Electronic effects of icosahedral carboranes: kinetic evidence for interaction between boron atom and nucleophile in the solvolysis of ( o-carboranyl)benzyl tosylates
Published in Tetrahedron letters (03-09-2001)“…Solvolysis of ( o-, m- and p-carboranyl)benzyl toluene- p-sulfonates substituted at the second carbon atom with a phenyl group bearing a range of substituents…”
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Discovery of S‑217622, a Noncovalent Oral SARS-CoV‑2 3CL Protease Inhibitor Clinical Candidate for Treating COVID-19
Published in Journal of medicinal chemistry (12-05-2022)“…The coronavirus disease 2019 (COVID-19) pandemic, caused by severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), has resulted in millions of deaths…”
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Structure-activity relationship studies of anti-bunyaviral cap-dependent endonuclease inhibitors
Published in Bioorganic & medicinal chemistry letters (01-03-2023)“…[Display omitted] Bunyaviruses, including the Lassa virus (LASV), are known to cause hemorrhagic fever and have a high fatality rate among hospitalized…”
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Electronic effects of icosahedral carboranes. Friedel-Crafts acylation of 1-phenyl-1,2-, 1,7-, and 1,12-dicarba- closo-dodecaboranes
Published in Tetrahedron letters (17-12-1999)“…Friedel-Crafts acylation of the benzene nucleus of 1-phenyl-1,2-, 1,7- and 1,12-dicarba- closo-dodecaboranes (phenylcarboranes) proceeded in the presence of…”
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Discovery of novel HIV-1 integrase-LEDGF/p75 allosteric inhibitors based on a pyridine scaffold forming an intramolecular hydrogen bond
Published in Bioorganic & medicinal chemistry letters (01-02-2021)“…[Display omitted] We have discovered HIV-1 novel integrase-LEDGF/p75 allosteric inhibitors (INLAIs) based on a pyridine scaffold forming an intramolecular…”
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Dihydrodibenzothiepine: Promising hydrophobic pharmacophore in the influenza cap-dependent endonuclease inhibitor
Published in Bioorganic & medicinal chemistry letters (15-11-2020)“…[Display omitted] This work describes a set of discovery research studies of an influenza cap-dependent endonuclease (CEN) inhibitor with a carbamoyl pyridone…”
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Molecular design and evaluation of aza-polycyclic carbamoyl pyridones as HIV-1 integrase strand transfer inhibitors
Published in Bioorganic & medicinal chemistry letters (01-10-2024)“…[Display omitted] Integrase strand transfer inhibitors (INSTIs) are the most prescribed anchor drug in antiretroviral therapy. Today, there is an increasing…”
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Carbamoyl Pyridone HIV‑1 Integrase Inhibitors 3. A Diastereomeric Approach to Chiral Nonracemic Tricyclic Ring Systems and the Discovery of Dolutegravir (S/GSK1349572) and (S/GSK1265744)
Published in Journal of medicinal chemistry (25-07-2013)“…We report herein the discovery of the human immunodeficiency virus type-1 (HIV-1) integrase inhibitors dolutegravir (S/GSK1349572) (3) and S/GSK1265744 (4)…”
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Synthesis and SAR Study of Carbamoyl Pyridone Bicycle Derivatives as Potent Inhibitors of Influenza Cap-dependent Endonuclease
Published in Journal of medicinal chemistry (12-09-2019)“…The medicinal chemistry and structure–activity relationships (SAR) for a novel series of carbamoyl pyridone bicycle (CAB) compounds as influenza Cap-dependent…”
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Discovery of tricyclic HIV-1 integrase-LEDGF/p75 allosteric inhibitors by intramolecular direct arylation reaction
Published in Bioorganic & medicinal chemistry letters (15-05-2022)“…[Display omitted] We have been conducting exploratory research to develop human immunodeficiency virus type-1 (HIV-1) integrase-LEDGF/p75 allosteric inhibitors…”
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Identification of cap-dependent endonuclease inhibitors with broad-spectrum activity against bunyaviruses
Published in Proceedings of the National Academy of Sciences - PNAS (06-09-2022)“…Viral hemorrhagic fevers caused by members of the order comprise endemic and emerging human infections that are significant public health concerns. Despite the…”
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Carbamoyl Pyridone HIV‑1 Integrase Inhibitors. 2. Bi- and Tricyclic Derivatives Result in Superior Antiviral and Pharmacokinetic Profiles
Published in Journal of medicinal chemistry (14-02-2013)“…This work is a continuation of our initial discovery of a potent monocyclic carbamoyl pyridone human immunodeficiency virus type-1 (HIV-1) integrase inhibitor…”
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Pyrrolinone derivatives as a new class of P2X3 receptor antagonists. Part 3: Structure-activity relationships of pyrropyrazolone derivatives
Published in Bioorganic & medicinal chemistry letters (15-12-2020)“…[Display omitted] •Pyrropyrazolone derivatives as a P2X3 receptor antagonist were synthesized.•The SAR studies were started from hit compound 3 with reference…”
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