Výsledky vyhledávání - "Brown, Jane T."

Akademický článek

Design and synthesis of a potent, highly selective, orally bioavailable, retinoic acid receptor alpha agonist

Autor: Clarke, Earl, Jarvis, Christopher I., Goncalves, Maria B., Kalindjian, S. Barret, Adams, David R., Brown, Jane T., Shiers, Jason J., Taddei, David M.A., Ravier, Elodie, Barlow, Stephanie, Miller, Iain, Smith, Vanessa, Borthwick, Alan D., Corcoran, Jonathan P.T.

Publikováno v: In Bioorganic & Medicinal Chemistry 15 February 2018 26(4):798-814

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Derivatisation of parthenolide to address chemoresistant chronic lymphocytic leukaemia† †Electronic supplementary information (ESI) available: General experimental details, aspects relating to cultivation of feverfew, the PTL extraction protocol, synthesis, biological assays computational information and spectrums are detailed in the supporting information. Methods described and references cited therein,45 should be referred to in regard of the docking, crystallographic, synthetic and toxicological studies detailed therein. See DOI: 10.1039/c9md00297a

Publikováno v: MedChemComm

A parthenolide-derivative with favourable pharmacokinetic properties and good activity against drug-resistant chronic lymphocytic leukaemia is reported.
Parthenolide is a natural product that exhibits anti-leukaemic activity, however, its clinic

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::ee5d2ad2f4324cc84079850240c3b333
http://europepmc.org/articles/PMC7478165

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Discovery and lead optimisation of a potent, selective and orally bioavailable RARβ agonist for the potential treatment of nerve injury

Autor: Goncalves, Maria B., Clarke, Earl, Jarvis, Christopher, Kalindjian, S. Barret, Pitcher, Thomas, Grist, John, Hobbs, Carl, Carlstedt, Thomas, Jack, Julian, Brown, Jane T., Mills, Mark, Mumford, Peter, Borthwick, Alan D., Corcoran, Jonathan P.T.

Publikováno v: Bioorganic & Medicinal Chemistry Letters
Goncalves, M B, Clarke, E, Jarvis, C, Kalindjian, S B, Pitcher, T, Grist, J, Hobbs, C, Carlstedt, T, Jack, J, Brown, J T, Mills, M, Mumford, P, Borthwick, A D & Corcoran, J P T 2019, ' Discovery and lead optimisation of a potent, selective and orally bioavailable RARβ agonist for the potential treatment of nerve injury ', Bioorganic & medicinal chemistry letters, vol. 29, no. 8, pp. 995-1000 . https://doi.org/10.1016/j.bmcl.2019.02.011

Graphical abstract
Oxadiazole replacement of an amide linkage in an RARα agonist template 1, followed by lead optimisation, has produced a highly potent and selective RARβ agonist 4-(5-(4,7-dimethylbenzofuran-2-yl)-1,2,4-oxadiazol-3-yl)benzoic

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid_dedup__::212eb1e845c6f4ef01aa7ee308576bc8
http://europepmc.org/articles/PMC6419571

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Design and synthesis of a potent, highly selective, orally bioavailable, retinoic acid receptor alpha agonist

Publikováno v: Clarke, E, Jarvis, C I, Goncalves, M B, Kalindjian, S B, Adams, D R, Brown, J T, Shiers, J J, Taddei, D M A, Ravier, E, Barlow, S, Miller, I, Smith, V, Borthwick, A D & Corcoran, J P T 2017, ' Design and synthesis of a potent, highly selective, orally bioavailable, retinoic acid receptor alpha agonist ', Bioorganic and Medicinal Chemistry . https://doi.org/10.1016/j.bmc.2017.12.015

A ligand-based virtual screening exercise examining likely bioactive conformations of AM 580 (2) and AGN 193836 (3) was used to identify the novel, less lipophilic RARα agonist 4-(3,5-dichloro-4-ethoxybenzamido)benzoic acid 5, which has good selecti

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=od______2761::4f01b85a6ae25d2064dcf50e0fa4e191
https://kclpure.kcl.ac.uk/ws/files/83192231/Design_and_synthesis_of_CLARKE_Publishedonline9December2017_GREEN_AAM_CC_BY_NC_ND_.pdf