Zobrazeno 1 - 10
of 26
pro vyhledávání: '"Fabrice Vergne"'
Autor:
Gary McCort, Rosalia Arrebola, Loreley Calvet, Baptiste Ronan, Fabrice Vergne, Francis Duffieux, Alexey Rak, Isabelle Meaux, David Papin, Florence Fassy, Cecile Delorme, Magali Matthieu, Jean-Paul Nicolas, Christophe Marcireau, Valerie Steier, Pierre-Yves Abecassis, Valerie Czepczor, Heather A. Thomson, Christopher D. Hupp, J.P. Guilinger, Ying Zhang, Anthony D. Keefe, John W. Cuozzo, Julie Liu, Laurent Debussche
Publikováno v:
Cancer Research. 79:3070-3070
From a screening of 27 106 covalent DNA-encoded compound library, a novel KRAS G12C chemical series has been identified. Original hit series compound displayed low µM covalent binding activity to KRAS G12C under GDP form associated with a k(inact)/K
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::cad2d9863f8a3a9d67e7a56774e2a777
https://doi.org/10.1158/1538-7445.am2019-3070
https://doi.org/10.1158/1538-7445.am2019-3070
Publikováno v:
Synlett. 2010:2913-2917
A polystyrene-supported α-aminonitrile has been prepared and its successive mono- and dialkylations achieved. Complementary procedures allow cleavage of the alkylated moities in either carbonyl or acetal form.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::0684cae0f9cfe7e8ec8979870395ea95
https://doi.org/10.1055/s-0030-1259032
https://doi.org/10.1055/s-0030-1259032
Autor:
Bernadette Bertin, Anita Tertre, Nga Pham, Françoise Berlioz-Seux, Moulay Idrissi, Patrick Bernardelli, Arnaud Descours, Edwige Lorthiois, Mei Li, Pierre Ducrot, Chrystelle Oliveira, Magali Coupe, François Moreau, Eric Chevalier, Fabrice Vergne, Emmanuelle Proust, Patrick Berna, Abdel-Kader Mafroud
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 14:4627-4631
The optimization of 5,8-disubstituted spirocyclohexane-quinazolinones into potent, selective, soluble PDE7 inhibitors with acceptable in vivo pharmacokinetic parameters is presented.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::98b645e96fe4aad63c13696befaf5e5e
https://doi.org/10.1016/j.bmcl.2004.07.010
https://doi.org/10.1016/j.bmcl.2004.07.010
Autor:
Magali Coupe, Bernadette Bertin, Arnaud Descours, François Moreau, Patrick Bernardelli, Edwige Lorthiois, Patricia Soulard, Patrick Berna, Roger Wrigglesworth, Anita Tertre, Abdel-Kader Mafroud, Lamia Heuze, Emmanuelle Proust, Chrystelle Oliveira, Fabrice Vergne, Moulay Idrissi
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 14:4623-4626
The synthesis and SAR studies of spiroquinazolinones as novel PDE7 inhibitors are discussed. The best compounds from the series displayed nanomolar inhibitory affinity and were selective versus other PDE isoenzymes.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fe38a476d80dbc5773e675bdb38f8ed6
https://doi.org/10.1016/j.bmcl.2004.07.011
https://doi.org/10.1016/j.bmcl.2004.07.011
Autor:
Ajith C Manage, Roger Wrigglesworth, Patrick Bernardelli, Edwige Lorthiois, Fabrice Vergne, Michael Bladon
Publikováno v:
Tetrahedron: Asymmetry. 15:1451-1455
(R,R)- and (S,S)-trans-3-Aminocyclohexanol were prepared via an enzymatic resolution of (±)-trans-1-acetoxy-3-benzylamido-cyclohexane with >95% enantiomeric excess.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::0f4e56b771bcf4bd043ea5539f8d3417
https://doi.org/10.1016/j.tetasy.2004.03.034
https://doi.org/10.1016/j.tetasy.2004.03.034
Publikováno v:
Journal of the Chemical Society, Perkin Transactions 1. :1681-1690
Chiral 2-(aminomethyl)oxazolines 3 and 7, in which the heterocycle is derived from (R)-phenylglycinol, are synthesized and studied in alkylation reactions involving strong base and alkyl halides. The tertiary amine derivative 3 is alkylated efficient
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::89dab8b8fe4871f81925b411541638c9
https://doi.org/10.1039/a608030h
https://doi.org/10.1039/a608030h
Publikováno v:
Tetrahedron. 52:2421-2428
A new synthesis of trans -1,2-diaminocyclobutane 1 is described, in which the key feature is the novel stereoselective borane-induced reductive ring-expansion reaction of the cyclopropane-iminonitrile 2 to give the cyclobutane 4 . This latter interme
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::c532fb3838a4bf9498d7b57c4bb74f12
https://doi.org/10.1016/0040-4020(95)01091-2
https://doi.org/10.1016/0040-4020(95)01091-2
Publikováno v:
ChemInform. 22
In the presence of lithium diisopropylamide at low temperature, the anion of the amino nitrile 1 is alkylated with epibromohydrin to give an acetonyl derivative 3; allene oxide is invoked as the reactive intermediate.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::a239f8fac84076c6afe96efa690e8fa9
https://doi.org/10.1002/chin.199132160
https://doi.org/10.1002/chin.199132160
Publikováno v:
ChemInform. 24
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::f39e5d9c3abb8aa185a5bccafb15acb3
https://doi.org/10.1002/chin.199309108
https://doi.org/10.1002/chin.199309108
Publikováno v:
ChemInform. 25
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::7e9999b8fe68c78ca35da2c0e3c16ef8
https://doi.org/10.1002/chin.199411059
https://doi.org/10.1002/chin.199411059