Synthesis of nucleotide analogues, EFdA, EdA and EdAP, and the effect of EdAP on hepatitis B virus replication

Design, Synthesis, and Biological Evaluation of EdAP, a 4′-Ethynyl-2′-Deoxyadenosine 5′-Monophosphate Analog, as a Potent Influenza a Inhibitor

(2019) Toshifumi Takeuchi et al.   MOLECULES

OUP accepted manuscript

(2018)   JOURNAL OF ANTIMICROBIAL CHEMOTHERAPY

4′-Ethynyl-2-fluoro-2′-deoxyadenosine, MK-8591

(2018) Martin Markowitz et al.   Current Opinion in HIV and AIDS

Enantioselective Synthesis of 4′-Ethynyl-2-fluoro-2′-deoxyadenosine (EFdA) via Enzymatic Desymmetrization

(2017) Mark McLaughlin et al.   ORGANIC LETTERS

Oral Administration of the Nucleoside EFdA (4′-Ethynyl-2-Fluoro-2′-Deoxyadenosine) Provides Rapid Suppression of HIV Viremia in Humanized Mice and Favorable Pharmacokinetic Properties in Mice and the Rhesus Macaque

(2015) Cheryl A. Stoddart et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

4′-modified nucleoside analogs: Potent inhibitors active against entecavir-resistant hepatitis B virus

(2015) Yuki Takamatsu et al.   HEPATOLOGY

Synthesis of EFdA via a Diastereoselective Aldol Reaction of a Protected 3-Keto Furanose

(2015) Kei Fukuyama et al.   ORGANIC LETTERS

Concise Synthesis of the Anti-HIV Nucleoside EFdA

(2015) Masayuki KAGEYAMA et al.   BIOSCIENCE BIOTECHNOLOGY AND BIOCHEMISTRY

Formation of covalently closed circular DNA in Hep38.7-Tet cells, a tetracycline inducible hepatitis B virus expression cell line

(2014) Naoki Ogura et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

4′-Ethynyl-2-fluoro-2′-deoxyadenosine (EFdA) Inhibits HIV-1 Reverse Transcriptase with Multiple Mechanisms

(2014) Eleftherios Michailidis et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Effects of Substitutions at the 4′ and 2 Positions on the Bioactivity of 4′-Ethynyl-2-Fluoro-2′-Deoxyadenosine

(2013) Karen A. Kirby et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Evaluation of Combinations of 4′-Ethynyl-2-Fluoro-2′-Deoxyadenosine with Clinically Used Antiretroviral Drugs

(2013) Atsuko Hachiya et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Delayed emergence of HIV-1 variants resistant to 4’-ethynyl-2-fluoro-2’-deoxyadenosine: comparative sequential passage study with lamivudine, tenofovir, emtricitabine and BMS-986001

(2013) Kenji Maeda et al.   ANTIVIRAL THERAPY

Evaluation and identification of hepatitis B virus entry inhibitors using HepG2 cells overexpressing a membrane transporter NTCP

(2013) Masashi Iwamoto et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

Preformulation studies of EFdA, a novel nucleoside reverse transcriptase inhibitor for HIV prevention

(2013) Wei Zhang et al.   DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY

Hypersusceptibility mechanism of Tenofovir-resistant HIV to EFdA

(2013) Eleftherios Michailidis et al.   Retrovirology

Response of Simian Immunodeficiency Virus to the Novel Nucleoside Reverse Transcriptase Inhibitor 4′-Ethynyl-2-Fluoro-2′-DeoxyadenosineIn VitroandIn Vivo

(2012) Michael Murphey-Corb et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Enantioselective Total Synthesis of the Potent Anti-HIV Nucleoside EFdA

(2011) Masayuki Kageyama et al.   ORGANIC LETTERS

Development of modified nucleosides that have supremely high anti-HIV activity and low toxicity and prevent the emergence of resistant HIV mutants

(2011) Hiroshi OHRUI   PROCEEDINGS OF THE JAPAN ACADEMY SERIES B-PHYSICAL AND BIOLOGICAL SCIENCES

Mechanism of Inhibition of HIV-1 Reverse Transcriptase by 4′-Ethynyl-2-fluoro-2′-deoxyadenosine Triphosphate, a Translocation-defective Reverse Transcriptase Inhibitor

(2009) Eleftherios Michailidis et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

2′-Deoxy-4′-C-ethynyl-2-halo-adenosines active against drug-resistant human immunodeficiency virus type 1 variants

(2008) Atsushi Kawamoto et al.   INTERNATIONAL JOURNAL OF BIOCHEMISTRY & CELL BIOLOGY