Výsledky vyhledávání

Virtual screening of the estrogen receptor

Autor: David Lloyd, Yidong Yang, Andrew J. S. Knox, Mary J. Meegan

Publikováno v: Expert Opinion on Drug Discovery. 3:853-866

For30 years, the estrogen receptor (ER) has been the most important biomarker in breast cancer, principally because of its role in indicating the potential of patients to benefit from endocrine therapy. The search for modulators of ER (selective estr

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1dbaead8994a8f7841ff20f8110ab6b2
https://doi.org/10.1517/17460441.3.8.853

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Lead identification of conformationally restricted β-lactam type combretastatin analogues : synthesis, antiproliferative activity and tubulin targeting effects

Autor: Miriam Carr, Daniela M. Zisterer, David Lloyd, Mary J. Meegan, Lisa M. Greene, Andrew J. S. Knox

The synthesis and study of the structureeactivity relationships of a series of rigid analogues of combretastatin A-4 are described which contain the 1,4-diaryl-2-azetidinone (β-lactam) ring system in place of the usual ethylene bridge present in the

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::83a3c801e9fa806ef9b032991fe28082
https://hdl.handle.net/1959.8/151898

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Lead identification of conformationally restricted benzoxepin type combretastatin analogs : synthesis, antiproliferative activity, and tubulin effects

Autor: Irene Barrett, David Lloyd, Mary J. Meegan, Andrew J. S. Knox, Lisa M. Greene, Miriam Carr, Daniela M. Zisterer, Niamh M. O’Boyle

We have synthesized a series of polymethoxylated rigid analogs of combretastatin A-4 which contain a benzoxepin ring in place of the usual ethylene bridge present in the natural combretastatin products. The compounds display antiproliferative activit

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::77f7372561ebd2eda29db4ea0b10699d
https://hdl.handle.net/1959.8/151734

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Synthesis and serotonin transporter activity of sulphur-substituted a-alkyl phenethylamines as a new class of anticancer agents

Autor: David Lloyd, Dilip K. Rai, Günther H.J. Peters, Andrew J. S. Knox, D. Clive Williams, Mary J. Meegan, Desmond Corrigan, Stephen Butler, John J. Keating, Suzanne M. Cloonan, Anne Marie Jørgensen

The discovery that some serotonin reuptake transporter (SERT) ligands have the potential to act as pro-apoptotic agents in the treatment of cancer adds greatly to their diverse pharmacological application. 4-Methylthioamphetamine (MTA) is a selective

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9c5c9407a4cae422094d639e7b81bc09
https://hdl.handle.net/1959.8/159978

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Akademický článek

Modulating the Blood-Brain Barrier: A Comprehensive Review.

Autor: Whelan R; School of Biological and Health Sciences, Technological University Dublin, Central Quad, Grangegorman, D07 XT95 Dublin, Ireland.; Chemical and Structural Biology, Environmental Sustainability and Health Institute, Technological University Dublin, D07 H6K8 Dublin, Ireland., Hargaden GC; School of Chemical and Pharmaceutical Sciences, Technological University Dublin, Central Quad, Grangegorman, D07 XT95 Dublin, Ireland., Knox AJS; School of Biological and Health Sciences, Technological University Dublin, Central Quad, Grangegorman, D07 XT95 Dublin, Ireland.; Chemical and Structural Biology, Environmental Sustainability and Health Institute, Technological University Dublin, D07 H6K8 Dublin, Ireland.

Publikováno v: Pharmaceutics [Pharmaceutics] 2021 Nov 22; Vol. 13 (11). Date of Electronic Publication: 2021 Nov 22.

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Akademický článek

Synthesis and optimisation of P 3 substituted vinyl sulfone-based inhibitors as anti-trypanosomal agents.

Autor: Doherty W; Centre for Synthesis and Chemical Biology, School of Chemistry and Chemical Biology, University College Dublin, Dublin D04 N2E2, Ireland., Adler N; School of Biochemistry and Immunology, Trinity Biomedical Sciences Institute, Trinity College Dublin, Pearse Street, Dublin 2, Ireland., Butler TJ; School of Biological and Health Sciences, Technological University Dublin, Dublin City Campus, Kevin St., Dublin D08 NF82, Ireland., Knox AJS; School of Biochemistry and Immunology, Trinity Biomedical Sciences Institute, Trinity College Dublin, Pearse Street, Dublin 2, Ireland; School of Biological and Health Sciences, Technological University Dublin, Dublin City Campus, Kevin St., Dublin D08 NF82, Ireland. Electronic address: andrew.knox@tudublin.ie., Evans P; Centre for Synthesis and Chemical Biology, School of Chemistry and Chemical Biology, University College Dublin, Dublin D04 N2E2, Ireland. Electronic address: paul.evans@ucd.ie.

Publikováno v: Bioorganic & medicinal chemistry [Bioorg Med Chem] 2020 Dec 01; Vol. 28 (23), pp. 115774. Date of Electronic Publication: 2020 Sep 20.

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