Zobrazeno 1 - 10
of 19
pro vyhledávání: '"Christine Lambert-van der Brempt"'
Autor:
Christine Lambert-van der Brempt, Jean-Jacques Marcel Lohmann, Twana Saleh, Sébastien L. Degorce, Stephen Green, Rémy Morgentin, Lara Ward, Urs Hancox, Mickaël Maudet, Martina Fitzek, Barlaam Bernard Christophe, Sabina Cosulich, Patrick Ple, Nicolas Warin, Aurélien Péru
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 26:2318-2323
We report the discovery and optimisation of a series of 8-(2,3-dihydro-1,4-benzoxazin-4-ylmethyl)-2-morpholino-4-oxo-chromene-6-carboxamides, leading to compound 16 as a potent and selective PI3Kβ/δ inhibitor: PI3Kβ cell IC50 0.012 μM (in PTEN nu
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::89c86409d445b8e16d247fcaa77b77b0
https://doi.org/10.1016/j.bmcl.2016.03.034
https://doi.org/10.1016/j.bmcl.2016.03.034
Autor:
Lara Ward, Stephen Green, Kevin Hudson, Martina Fitzek, Benedicte Delouvrie, Craig S. Harris, Linette Ruston, Christine Lambert-van der Brempt, Sabina Cosulich, Ken Page, Barlaam Bernard Christophe, Gilles Ouvry
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 25:2679-2685
Starting from compound 1, a potent PI3Kα inhibitor having poor general kinase selectivity, we used structural data and modelling to identify key exploitable differences between PI3Kα and the other kinases. This approach led us to design chemical mo
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::eebfcc07914b33e1b224ec523d7595ed
https://doi.org/10.1016/j.bmcl.2015.04.084
https://doi.org/10.1016/j.bmcl.2015.04.084
Autor:
Stephen Green, Sébastien L. Degorce, Sabina Cosulich, Martina Fitzek, Michel Vautier, Christine Lambert-van der Brempt, Lara Ward, Jean-Jacques Marcel Lohmann, Patrick Ple, Barlaam Bernard Christophe, Marie-Jeanne Pasquet, Rémy Morgentin, Michael A. Walker, Twana Saleh, Nicolas Warin, Aurélien Péru, Urs Hancox, Mickaël Maudet
Publikováno v:
Journal of Medicinal Chemistry. 58:943-962
Several studies have highlighted the dependency of PTEN deficient tumors to PI3Kβ activity and specific inhibition of PI3Kδ has been shown activity against human B-cell cancers. We describe the discovery and optimization of a series of 8-(1-anilino
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::374fddcd264180d79fb9424642feb5b5
https://doi.org/10.1021/jm501629p
https://doi.org/10.1021/jm501629p
Autor:
Rémy Morgentin, Martina Fitzek, Christine Lambert-van der Brempt, Stephen Green, Sébastien L. Degorce, Sabina Cosulich, Mickaël Maudet, Rebecca Ellston, Jean-Jacques Marcel Lohmann, Nicolas Warin, Urs Hancox, Patrick Ple, Lara Ward, Barlaam Bernard Christophe
Publikováno v:
Bioorganicmedicinal chemistry letters. 27(9)
Attempts to lock the active conformation of compound 4, a PI3Kβ/δ inhibitor (PI3Kβ cell IC50 0.015 μM), led to the discovery of a series of 8-(1-phenylpyrrolidin-2-yl)-6-carboxamide-2-morpholino-4H-chromen-4-ones, which showed high levels of pote
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9a1de19b5eb37f50e9906170d950d264
https://pubmed.ncbi.nlm.nih.gov/28347666
https://pubmed.ncbi.nlm.nih.gov/28347666
Autor:
Christine Lambert-van der Brempt, Barlaam Bernard Christophe, Sabina Cosulich, Lara Ward, Twana Saleh, Martina Fitzek, Fabrizio Giordanetto, Rémy Morgentin, Sébastien L. Degorce, Laurent Francois Andre Hennequin, Tord Inghardt, Urs Hancox, Patrick Ple, Sarah L. Pass, Stephen Green
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 24:3928-3935
Starting from TGX-221, we designed a series of 9-(1-anilinoethyl)-2-morpholino-4-oxo-pyrido[1,2-a]pyrimidine-7-carboxamides as potent and selective PI3Kβ/δ inhibitors. Structure–activity relationships and structure–property relationships around
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2957a67f99262704df92803e1f7edd0d
https://doi.org/10.1016/j.bmcl.2014.06.040
https://doi.org/10.1016/j.bmcl.2014.06.040
Autor:
Robert Hugh Bradbury, Cath Trigwell, John Vincent, Barlaam Bernard Christophe, Donald J. Ogilvie, George Kirk, Judith Anderton, Jason Grant Kettle, D. Mark Hickinson, Laurent Francois Andre Hennequin, Peter Ballard, Teresa Klinowska, Christine Lambert-van der Brempt
Publikováno v:
ACS Medicinal Chemistry Letters. 4:742-746
Deregulation of HER family signaling promotes proliferation and tumor cell survival and has been described in many human cancers. Simultaneous, equipotent inhibition of EGFR-, HER2-, and HER3-mediated signaling may be of clinical utility in cancer se
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5fa7f05bc63b1a8fbb191a888276a0ce
https://doi.org/10.1021/ml400146c
https://doi.org/10.1021/ml400146c
Autor:
Honorine Lebraud, Christine Lambert-van der Brempt, Paul R. J. Davey, Craig S. Harris, Sébastien L. Degorce, Myriam Didelot, Benedicte Delouvrie, Hervé Germain, Gilles Ouvry
Publikováno v:
Tetrahedron Letters. 53:6078-6082
Access to the 1,5-disubstituted-1 H -1,2,4-triazole-3-carboxamide motif is quite laborious and requires forcing conditions to effect the cyclocondensation step. Herein, we report an efficient and mild one-pot protocol to access this substructure in g
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::f07a38dbdd0894dbc8e27b3d34e478c5
https://doi.org/10.1016/j.tetlet.2012.08.130
https://doi.org/10.1016/j.tetlet.2012.08.130
Autor:
Simon T. Barry, A. Hughes, Craig S. Harris, Martin Pass, Benedicte Delouvrie, Jane Kendrew, Michel Vautier, David A. Jude, Hervé Germain, Myriam Didelot, Jean-Jacques Marcel Lohmann, Jean-Claude Arnould, Andrew A. Mortlock, Nicolas Warin, Jennifer L. Vincent, Katherine Al-Kadhimi, Paul R. Gavine, Morgan Ménard, Christine Lambert-van der Brempt, Darren Cross, Claire Rooney
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:4117-4121
Potent antagonists of the integrin ?(5)?(1), which are RGD mimetics built from tyrosine are described. This letter describes the optimization of in vitro potency obtained by variation of two parts of the molecule, the basic group and the linker betwe
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::930317b9e878eee93e46746ef6da9c53
https://doi.org/10.1016/j.bmcl.2012.04.061
https://doi.org/10.1016/j.bmcl.2012.04.061
Autor:
Bénédicte, Delouvrié, Katherine, Al-Kadhimi, Jean-Claude, Arnould, Simon T, Barry, Darren A E, Cross, Myriam, Didelot, Paul R, Gavine, Hervé, Germain, Craig S, Harris, Adina M, Hughes, David A, Jude, Jane, Kendrew, Christine, Lambert-van der Brempt, Jean-Jacques, Lohmann, Morgan, Ménard, Andrew A, Mortlock, Martin, Pass, Claire, Rooney, Michel, Vautier, Jennifer L, Vincent, Nicolas, Warin
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:4111-4116
Potent antagonists of the integrin α(5)β(1), which are RGD mimetics built from tyrosine are described. This letter describes the optimization of in vitro potency obtained by variation of two parts of the molecule, the basic group and the linker bet
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0461240ea9358c4597b4752286cf8269
https://doi.org/10.1016/j.bmcl.2012.04.063
https://doi.org/10.1016/j.bmcl.2012.04.063
Autor:
Patrick Ple, Frederic Henri Jung, Georges Rene Pasquet, Christine Lambert-van der Brempt, Sue Ashton, Taylor Sian Tomiko, Rémy Morgentin, Romuald Laine, Laurent Francois Andre Hennequin
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:3050-3055
A new series of quinoline ether inhibitors, which potently and selectively inhibit PDGFR tyrosine kinases, is described in this Letter. Compounds 23 and 33 are selective, low nanomolar inhibitors of PDGFRα and β, display good pharmacokinetics in ra
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::cd0a0f5d4453633b74b0f5d2c9fecb6e
https://doi.org/10.1016/j.bmcl.2012.03.074
https://doi.org/10.1016/j.bmcl.2012.03.074