Zobrazeno 1 - 10
of 30
pro vyhledávání: '"Eric, Ferrandis"'
Autor:
Ernest Hamel, Pascoe Mannion, Grégory Menchon, Mathew P. Leese, Michel O. Steinmetz, Philip G. Kasprzyk, Mark P. Thomas, Eric Ferrandis, Barry V. L. Potter, Fabrice Jourdan, Paul A. Foster, Andrea E. Prota, Wolfgang Dohle
Publikováno v:
Journal of Medicinal Chemistry. 61:1031-1044
Quinazolinone-based anti-cancer agents were designed, decorated with functional groups from a 2-methoxyestradiol-based microtubule disruptor series, incorporating the aryl sulfamate motif of steroid sulfatase (STS) inhibitors. The steroidal AB-ring s
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::66a2cfd9fa7b18e19c31a4bfb1e2c49f
https://doi.org/10.1021/acs.jmedchem.7b01474
https://doi.org/10.1021/acs.jmedchem.7b01474
Autor:
Ernest Hamel, Ann Fiore, Simon P. Newman, Ruoli Bai, Mathew P. Leese, Meriel R. Major, Fabrice Jourdan, Philip G. Kasprzyk, Wolfgang Dohle, Eric Ferrandis, Atul Purohit, Barry V. L. Potter
Publikováno v:
ChemMedChem. 9:350-370
The syntheses and antiproliferative activities of novel substituted tetrahydroisoquinoline derivatives and their sulfamates are discussed. Biasing of conformational populations through substitution on the tetrahydroisoquinoline core at C1 and C3 has
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4704a75c99b657f197a8b9002766f84c
https://doi.org/10.1002/cmdc.201300412
https://doi.org/10.1002/cmdc.201300412
Autor:
Fabrice Jourdan, Eric Ferrandis, Meriel R. Kimberley, Ernest Hamel, Barry V. L. Potter, Ruoli Bai, Wolfgang Dohle, Mathew P. Leese, Mark P. Thomas
Publikováno v:
ACS Medicinal Chemistry Letters
Structure–activity relationship translation offers an expeditious means for discovery of new active series. This approach was applied to discover tetrahydroisoquinoline (THIQ)-based steroidomimetic microtubule disruptors. The two A-ring elements of
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::cff378e055e453c0255790db93281078
https://doi.org/10.1021/ml200232c
https://doi.org/10.1021/ml200232c
Structure–Activity Relationships of C-17-Substituted Estratriene-3-O-sulfamates as Anticancer Agents
Autor:
Simon P. Newman, Fabrice Jourdan, Surinder K. Chander, Atul Purohit, Eric Ferrandis, Barry V. L. Potter, Wolfgang Dohle, Mathew P. Leese
Publikováno v:
Journal of Medicinal Chemistry. 54:4863-4879
The synthesis and antiproliferative activities of analogues of 2-substituted estradiol-3,17-O,O-bis-sulfamates (E2bisMATEs) are discussed. Modifications of the C-17 substituent confirm that an H-bond acceptor is essential for high activity; its optim
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c81d2db41d81728733032b64f8149a47
https://doi.org/10.1021/jm200483x
https://doi.org/10.1021/jm200483x
Autor:
S. Pradhananga, Ian Wilkinson, Jon R. Sayers, Caroline Touvay, Peter J. Artymiuk, Carol Kinoshita, Eric Ferrandis, Zida Wu, Kevin Stafford, Christian J. Strasburger, Richard J. Ross
Publikováno v:
Clinical Science. 119:483-491
A fundamental concern for all new biological therapeutics is the possibility of inducing an immune response. We have recently demonstrated that an LR-fusion (ligand–receptor fusion) of growth hormone generates a potent long-acting agonist; however,
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::52cd8f90a7988d8016b891e8545a1be6
https://doi.org/10.1042/cs20100241
https://doi.org/10.1042/cs20100241
Autor:
Simon P. Newman, Fabrice Jourdan, Barry V. L. Potter, Mathew P. Leese, Eric Ferrandis, Ernest Hamel, Atul Purohit, Wolfgang Dohle, Michael J. Reed
Publikováno v:
Journal of Medicinal Chemistry. 53:2942-2951
The synthesis and antiproliferative activity of analogues of estradiol 3,17-O,O-bis-sulfamates (E2bisMATEs) are discussed. Modifications of the C-17 substituent reveal that an H-bond acceptor is essential for high antiproliferative activity. The loca
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1b2d8de42356653eeea337adeff04475
https://doi.org/10.1021/jm9018806
https://doi.org/10.1021/jm9018806
Autor:
Dennis Bigg, Simon P. Newman, Chloe Stengel, Sonia Bernetiere, Raphael Dellile, Mark Carlson, José Camara, Eric Ferrandis, Mélissa Le Moing, Nadine Narboux, Vincent Hesry, Delphine Morlais, Olivier Dutruel, Dominique Pons, Pierrick Auvray, Anne-Marie Liberatore, Philip G. Kasprzyk, Hélène Coulomb, Ann Savola Nelson, Béatrice Foll, Gregoire Prevost
Publikováno v:
Molecular Cancer Therapeutics. 7:2426-2434
Tubulin is a validated target for antitumor drugs. However, the effectiveness of these microtubule-interacting agents is limited by the fact that they are substrates for drug efflux pumps (P-glycoprotein) and/or by the acquisition of point mutations
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d1e8e70f3246309738f21d393b63bf5b
https://doi.org/10.1158/1535-7163.mct-08-0208
https://doi.org/10.1158/1535-7163.mct-08-0208
Autor:
Gregoire Prevost, Pierre Roubert, Daniel W. Zaharevitz, Marie Odile Lonchampt, Samir Attoub, Sophie Chaumeron, Mike Alley, Erik Bruyneel, Hélène Coulomb, Ann Savola, Philip G. Kasprzyk, Susan Holbeck, John Wright, Quang-Dé Nguyen, Patricia Forgez, Christian Gespach, Marie C. Brezak, Mark Bracke, Eric Ferrandis, Marion Huchet, Danièle Demarquay
Publikováno v:
Cancer Research. 66:9227-9234
A large number of hormones and local agonists activating guanine-binding protein-coupled receptors (GPCR) play a major role in cancer progression. Here, we characterize the new imidazo-pyrazine derivative BIM-46174, which acts as a selective inhibito
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::7e35e09855de720491c38a3f5fd371a5
https://doi.org/10.1158/0008-5472.can-05-4205
https://doi.org/10.1158/0008-5472.can-05-4205
Autor:
Eric Ferrandis, Ernest Hamel, Wolfgang Dohle, Mathew P. Leese, Barry V. L. Potter, Fabrice Jourdan, Christopher J. Chapman
Publikováno v:
ChemMedChem.
Tetrahydroisoquinoline (THIQ)-based “chimeric” microtubule disruptors were optimised through modification of the N-benzyl motif, in concert with changes at C3 and C7, resulting in the identification of compounds with improved in vitro antiprolife
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0b51a082153871575bab79ada6e215ac
https://doi.org/10.1002/cmdc.201402025
https://doi.org/10.1002/cmdc.201402025
Autor:
Ernest Hamel, Mathew P. Leese, Eric Ferrandis, Ann Fiore, Philip G. Kasprzyk, Wolfgang Dohle, Meriel R. Major, Fabrice Jourdan, Barry V. L. Potter
A structure–activity relationship (SAR) translation strategy was used for the discovery of tetrahydroisoquinoline (THIQ)-based steroidomimetic and chimeric microtubule disruptors based upon a steroidal starting point. A steroid A,B-ring-mimicking T
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::abd948869e61c3583d284f7237f6c5d9
https://europepmc.org/articles/PMC3877212/
https://europepmc.org/articles/PMC3877212/
