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

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

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: 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

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Structure and property based design of factor Xa inhibitors: pyrrolidin-2-ones with monoaryl P4 motifs

Autor: Kleanthous, Savvas, Borthwick, Alan D., Brown, David, Burns-Kurtis, Cynthia L., Campbell, Matthew, Chaudry, Laiq, Chan, Chuen, Clarte, Marie-Olive, Convery, Máire A., Harling, John D., Hortense, Eric, Irving, Wendy R., Irvine, Stephanie, Pateman, Anthony J., Patikis, Angela N., Pinto, Ivan L., Pollard, Derek R., Roethka, Theresa J., Senger, Stefan, Shah, Gita P., Stelman, Gary J., Toomey, John R., Watson, Nigel S., West, Robert I., Whittaker, Caroline, Zhou, Ping, Young, Robert J.

Publikováno v: In Bioorganic & Medicinal Chemistry Letters 2010 20(2):618-622