AiZynth impact on medicinal chemistry practice at AstraZeneca.

Autor: Shields JD; Early Oncology R&D, AstraZeneca 35 Gatehouse Drive Waltham MA 02451 USA jason.shields@astrazeneca.com., Howells R; Early Oncology R&D, AstraZeneca 1 Francis Crick Avenue Cambridge CB2 0AA UK., Lamont G; Early Oncology R&D, AstraZeneca 1 Francis Crick Avenue Cambridge CB2 0AA UK., Leilei Y; Pharmaron Beijing Co., Ltd. 6 Taihe Road BDA Beijing 100176 P.R. China., Madin A; Discovery Sciences, AstraZeneca 1 Francis Crick Avenue Cambridge CB2 0AA UK., Reimann CE; Early Oncology R&D, AstraZeneca 35 Gatehouse Drive Waltham MA 02451 USA jason.shields@astrazeneca.com., Rezaei H; Early Oncology R&D, AstraZeneca 35 Gatehouse Drive Waltham MA 02451 USA jason.shields@astrazeneca.com., Reuillon T; Respiratory & Immunology, BioPharmaceuticals R&D, AstraZeneca Pepparedsleden 1 43183 Mölndal Sweden., Smith B; Early Oncology R&D, AstraZeneca 1 Francis Crick Avenue Cambridge CB2 0AA UK., Thomson C; Early Oncology R&D, AstraZeneca 1 Francis Crick Avenue Cambridge CB2 0AA UK., Zheng Y; Pharmaron Beijing Co., Ltd. 6 Taihe Road BDA Beijing 100176 P.R. China., Ziegler RE; Early Oncology R&D, AstraZeneca 35 Gatehouse Drive Waltham MA 02451 USA jason.shields@astrazeneca.com.

Publikováno v: RSC medicinal chemistry [RSC Med Chem] 2024 Feb 16; Vol. 15 (4), pp. 1085-1095. Date of Electronic Publication: 2024 Feb 16 (Print Publication: 2024).

Parallel Optimization of Potency and Pharmacokinetics Leading to the Discovery of a Pyrrole Carboxamide ERK5 Kinase Domain Inhibitor.

Autor: Miller DC; Cancer Research UK Newcastle Drug Discovery Unit, Newcastle University Centre for Cancer, School of Natural and Environmental Sciences, Bedson Building, Newcastle University, Newcastle upon Tyne NE1 7RU, U.K., Reuillon T; Cancer Research UK Newcastle Drug Discovery Unit, Newcastle University Centre for Cancer, School of Natural and Environmental Sciences, Bedson Building, Newcastle University, Newcastle upon Tyne NE1 7RU, U.K., Molyneux L; Cancer Research UK Newcastle Drug Discovery Unit, Newcastle University Centre for Cancer, School of Natural and Environmental Sciences, Bedson Building, Newcastle University, Newcastle upon Tyne NE1 7RU, U.K., Blackburn T; Cancer Research UK Newcastle Drug Discovery Unit, Newcastle University Centre for Cancer, School of Natural and Environmental Sciences, Bedson Building, Newcastle University, Newcastle upon Tyne NE1 7RU, U.K., Cook SJ; Signalling Laboratory, The Babraham Institute, Babraham Research Campus, Cambridge CB22 3AT, U.K., Edwards N; Cancer Research UK Newcastle Drug Discovery Unit, Newcastle University Centre for Cancer, Paul O'Gorman Building, Medical School, Framlington Place, Newcastle upon Tyne NE2 4HH, U.K., Endicott JA; Cancer Research UK Newcastle Drug Discovery Unit, Newcastle University Centre for Cancer, Paul O'Gorman Building, Medical School, Framlington Place, Newcastle upon Tyne NE2 4HH, U.K., Golding BT; Cancer Research UK Newcastle Drug Discovery Unit, Newcastle University Centre for Cancer, School of Natural and Environmental Sciences, Bedson Building, Newcastle University, Newcastle upon Tyne NE1 7RU, U.K., Griffin RJ; Cancer Research UK Newcastle Drug Discovery Unit, Newcastle University Centre for Cancer, School of Natural and Environmental Sciences, Bedson Building, Newcastle University, Newcastle upon Tyne NE1 7RU, U.K., Hardcastle I; Cancer Research UK Newcastle Drug Discovery Unit, Newcastle University Centre for Cancer, School of Natural and Environmental Sciences, Bedson Building, Newcastle University, Newcastle upon Tyne NE1 7RU, U.K., Harnor SJ; Cancer Research UK Newcastle Drug Discovery Unit, Newcastle University Centre for Cancer, School of Natural and Environmental Sciences, Bedson Building, Newcastle University, Newcastle upon Tyne NE1 7RU, U.K., Heptinstall A; Cancer Research UK Newcastle Drug Discovery Unit, Newcastle University Centre for Cancer, School of Natural and Environmental Sciences, Bedson Building, Newcastle University, Newcastle upon Tyne NE1 7RU, U.K., Lochhead P; Signalling Laboratory, The Babraham Institute, Babraham Research Campus, Cambridge CB22 3AT, U.K., Martin MP; Cancer Research UK Newcastle Drug Discovery Unit, Newcastle University Centre for Cancer, Paul O'Gorman Building, Medical School, Framlington Place, Newcastle upon Tyne NE2 4HH, U.K., Martin NC; Cancer Research UK Newcastle Drug Discovery Unit, Newcastle University Centre for Cancer, School of Natural and Environmental Sciences, Bedson Building, Newcastle University, Newcastle upon Tyne NE1 7RU, U.K., Myers S; Cancer Research UK Newcastle Drug Discovery Unit, Newcastle University Centre for Cancer, School of Natural and Environmental Sciences, Bedson Building, Newcastle University, Newcastle upon Tyne NE1 7RU, U.K., Newell DR; Cancer Research UK Newcastle Drug Discovery Unit, Newcastle University Centre for Cancer, Paul O'Gorman Building, Medical School, Framlington Place, Newcastle upon Tyne NE2 4HH, U.K., Noble RA; Cancer Research UK Newcastle Drug Discovery Unit, Newcastle University Centre for Cancer, Paul O'Gorman Building, Medical School, Framlington Place, Newcastle upon Tyne NE2 4HH, U.K., Phillips N; Cancer Research UK Newcastle Drug Discovery Unit, Newcastle University Centre for Cancer, Paul O'Gorman Building, Medical School, Framlington Place, Newcastle upon Tyne NE2 4HH, U.K., Rigoreau L; Cancer Research UK Therapeutic Discovery Laboratories, Jonas Webb Building, Babraham Campus, Babraham, Cambridgeshire CB22 3AT, U.K., Thomas H; Cancer Research UK Newcastle Drug Discovery Unit, Newcastle University Centre for Cancer, Paul O'Gorman Building, Medical School, Framlington Place, Newcastle upon Tyne NE2 4HH, U.K., Tucker JA; Cancer Research UK Newcastle Drug Discovery Unit, Newcastle University Centre for Cancer, Paul O'Gorman Building, Medical School, Framlington Place, Newcastle upon Tyne NE2 4HH, U.K., Wang LZ; Cancer Research UK Newcastle Drug Discovery Unit, Newcastle University Centre for Cancer, Paul O'Gorman Building, Medical School, Framlington Place, Newcastle upon Tyne NE2 4HH, U.K., Waring MJ; Cancer Research UK Newcastle Drug Discovery Unit, Newcastle University Centre for Cancer, School of Natural and Environmental Sciences, Bedson Building, Newcastle University, Newcastle upon Tyne NE1 7RU, U.K., Wong AC; Cancer Research UK Therapeutic Discovery Laboratories, London Bioscience Innovation Centre, 2 Royal College Street, London NW1 0NH, U.K., Wedge SR; Cancer Research UK Newcastle Drug Discovery Unit, Newcastle University Centre for Cancer, Paul O'Gorman Building, Medical School, Framlington Place, Newcastle upon Tyne NE2 4HH, U.K., Noble MEM; Cancer Research UK Newcastle Drug Discovery Unit, Newcastle University Centre for Cancer, Paul O'Gorman Building, Medical School, Framlington Place, Newcastle upon Tyne NE2 4HH, U.K., Cano C; Cancer Research UK Newcastle Drug Discovery Unit, Newcastle University Centre for Cancer, School of Natural and Environmental Sciences, Bedson Building, Newcastle University, Newcastle upon Tyne NE1 7RU, U.K.

Publikováno v: Journal of medicinal chemistry [J Med Chem] 2022 May 12; Vol. 65 (9), pp. 6513-6540. Date of Electronic Publication: 2022 Apr 25.

Identification of a novel orally bioavailable ERK5 inhibitor with selectivity over p38α and BRD4.

Autor: Myers SM; Newcastle Drug Discovery, Northern Institute for Cancer Research, School of Chemistry, Bedson Building, Newcastle University, Newcastle Upon Tyne, NE1 7RU, UK., Miller DC; Newcastle Drug Discovery, Northern Institute for Cancer Research, School of Chemistry, Bedson Building, Newcastle University, Newcastle Upon Tyne, NE1 7RU, UK., Molyneux L; Newcastle Drug Discovery, Northern Institute for Cancer Research, School of Chemistry, Bedson Building, Newcastle University, Newcastle Upon Tyne, NE1 7RU, UK., Arasta M; Newcastle Drug Discovery, Northern Institute for Cancer Research, Paul O'Gorman Building, Medical School, Framlington Place, Newcastle Upon Tyne, NE2 4HH, UK., Bawn RH; Newcastle Drug Discovery, Northern Institute for Cancer Research, School of Chemistry, Bedson Building, Newcastle University, Newcastle Upon Tyne, NE1 7RU, UK., Blackburn TJ; Newcastle Drug Discovery, Northern Institute for Cancer Research, School of Chemistry, Bedson Building, Newcastle University, Newcastle Upon Tyne, NE1 7RU, UK., Cook SJ; Signalling Laboratory, The Babraham Institute, Babraham Research Campus, Cambridge, CB22 3AT, UK., Edwards N; Newcastle Drug Discovery, Northern Institute for Cancer Research, Paul O'Gorman Building, Medical School, Framlington Place, Newcastle Upon Tyne, NE2 4HH, UK., Endicott JA; Newcastle Drug Discovery, Northern Institute for Cancer Research, Paul O'Gorman Building, Medical School, Framlington Place, Newcastle Upon Tyne, NE2 4HH, UK., Golding BT; Newcastle Drug Discovery, Northern Institute for Cancer Research, School of Chemistry, Bedson Building, Newcastle University, Newcastle Upon Tyne, NE1 7RU, UK., Griffin RJ; Newcastle Drug Discovery, Northern Institute for Cancer Research, School of Chemistry, Bedson Building, Newcastle University, Newcastle Upon Tyne, NE1 7RU, UK., Hammonds T; Cancer Research UK Therapeutic Discovery Laboratories, London Bioscience Innovation Centre, 2 Royal College Street, London, NW1 0NH, UK., Hardcastle IR; Newcastle Drug Discovery, Northern Institute for Cancer Research, School of Chemistry, Bedson Building, Newcastle University, Newcastle Upon Tyne, NE1 7RU, UK., Harnor SJ; Newcastle Drug Discovery, Northern Institute for Cancer Research, School of Chemistry, Bedson Building, Newcastle University, Newcastle Upon Tyne, NE1 7RU, UK., Heptinstall AB; Newcastle Drug Discovery, Northern Institute for Cancer Research, School of Chemistry, Bedson Building, Newcastle University, Newcastle Upon Tyne, NE1 7RU, UK., Lochhead PA; Signalling Laboratory, The Babraham Institute, Babraham Research Campus, Cambridge, CB22 3AT, UK., Martin MP; Newcastle Drug Discovery, Northern Institute for Cancer Research, Paul O'Gorman Building, Medical School, Framlington Place, Newcastle Upon Tyne, NE2 4HH, UK., Martin NC; Newcastle Drug Discovery, Northern Institute for Cancer Research, School of Chemistry, Bedson Building, Newcastle University, Newcastle Upon Tyne, NE1 7RU, UK., Newell DR; Newcastle Drug Discovery, Northern Institute for Cancer Research, Paul O'Gorman Building, Medical School, Framlington Place, Newcastle Upon Tyne, NE2 4HH, UK., Owen PJ; Cancer Research UK Therapeutic Discovery Laboratories, London Bioscience Innovation Centre, 2 Royal College Street, London, NW1 0NH, UK., Pang LC; Cancer Research UK Therapeutic Discovery Laboratories, London Bioscience Innovation Centre, 2 Royal College Street, London, NW1 0NH, UK., Reuillon T; Newcastle Drug Discovery, Northern Institute for Cancer Research, School of Chemistry, Bedson Building, Newcastle University, Newcastle Upon Tyne, NE1 7RU, UK., Rigoreau LJM; Cancer Research UK Therapeutic Discovery Laboratories, Jonas Webb Building, Babraham Campus, Babraham, Cambridgeshire, CB22 3AT, UK., Thomas HD; Newcastle Drug Discovery, Northern Institute for Cancer Research, Paul O'Gorman Building, Medical School, Framlington Place, Newcastle Upon Tyne, NE2 4HH, UK., Tucker JA; Newcastle Drug Discovery, Northern Institute for Cancer Research, Paul O'Gorman Building, Medical School, Framlington Place, Newcastle Upon Tyne, NE2 4HH, UK., Wang LZ; Newcastle Drug Discovery, Northern Institute for Cancer Research, Paul O'Gorman Building, Medical School, Framlington Place, Newcastle Upon Tyne, NE2 4HH, UK., Wong AC; Cancer Research UK Therapeutic Discovery Laboratories, London Bioscience Innovation Centre, 2 Royal College Street, London, NW1 0NH, UK., Noble MEM; Newcastle Drug Discovery, Northern Institute for Cancer Research, Paul O'Gorman Building, Medical School, Framlington Place, Newcastle Upon Tyne, NE2 4HH, UK. Electronic address: martin.noble@ncl.ac.uk., Wedge SR; Newcastle Drug Discovery, Northern Institute for Cancer Research, Paul O'Gorman Building, Medical School, Framlington Place, Newcastle Upon Tyne, NE2 4HH, UK. Electronic address: steve.wedge@ncl.ac.uk., Cano C; Newcastle Drug Discovery, Northern Institute for Cancer Research, School of Chemistry, Bedson Building, Newcastle University, Newcastle Upon Tyne, NE1 7RU, UK. Electronic address: celine.cano@ncl.ac.uk.

Publikováno v: European journal of medicinal chemistry [Eur J Med Chem] 2019 Sep 15; Vol. 178, pp. 530-543. Date of Electronic Publication: 2019 May 25.

The Capacity of Drug-Metabolising Enzymes in Modulating the Therapeutic Efficacy of Drugs to Treat Rhabdomyosarcoma.

Autor: Picher, Enric Arasanz¹ (AUTHOR) earasanz@bradford.ac.uk, Wahajuddin, Muhammad¹ (AUTHOR) m.wahajuddin@bradford.ac.uk, Barth, Stefan² (AUTHOR) stefan.barth@uct.ac.za, Chisholm, Julia³ (AUTHOR) julia.chisholm@rmh.nhs.uk, Shipley, Janet⁴ (AUTHOR) janet.shipley@icr.ac.uk, Pors, Klaus¹ (AUTHOR) k.pors1@bradford.ac.uk

Publikováno v: Cancers. Mar2024, Vol. 16 Issue 5, p1012. 22p.

AMPA Receptor Positive Allosteric Modulators: Potential for the Treatment of Neuropsychiatric and Neurological Disorders.

Autor: Reuillon T; Sussex Drug Discovery Centre, School of Life Sciences, University of Sussex, Falmer, Brighton, BN1 9QJ, UK. t.reuillon@sussex.ac.uk., Ward SE, Beswick P

Publikováno v: Current topics in medicinal chemistry [Curr Top Med Chem] 2016; Vol. 16 (29), pp. 3536-3565.