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Page 1
In vitro ion channel profile and ex vivo cardiac electrophysiology properties of the R(-) and S(+) enantiomers of hydroxychloroquine.
Ballet V, Bohme GA, Brohan E, Boukaiba R, Chambard JM, Angouillant-Boniface O, Carriot T, Chantoiseau C, Fouconnier S, Houtmann S, Prévost C, Schombert B, Schio L, Partiseti M. Ballet V, et al. Among authors: schio l. Eur J Pharmacol. 2022 Jan 15;915:174670. doi: 10.1016/j.ejphar.2021.174670. Epub 2021 Dec 2. Eur J Pharmacol. 2022. PMID: 34863995 Free PMC article.
Discovery and optimization of new benzimidazole- and benzoxazole-pyrimidone selective PI3Kβ inhibitors for the treatment of phosphatase and TENsin homologue (PTEN)-deficient cancers.
Certal V, Halley F, Virone-Oddos A, Delorme C, Karlsson A, Rak A, Thompson F, Filoche-Rommé B, El-Ahmad Y, Carry JC, Abecassis PY, Lejeune P, Vincent L, Bonnevaux H, Nicolas JP, Bertrand T, Marquette JP, Michot N, Benard T, Below P, Vade I, Chatreaux F, Lebourg G, Pilorge F, Angouillant-Boniface O, Louboutin A, Lengauer C, Schio L. Certal V, et al. Among authors: schio l. J Med Chem. 2012 May 24;55(10):4788-805. doi: 10.1021/jm300241b. Epub 2012 May 2. J Med Chem. 2012. PMID: 22524426
SAR156497, an exquisitely selective inhibitor of aurora kinases.
Carry JC, Clerc F, Minoux H, Schio L, Mauger J, Nair A, Parmantier E, Le Moigne R, Delorme C, Nicolas JP, Krick A, Abécassis PY, Crocq-Stuerga V, Pouzieux S, Delarbre L, Maignan S, Bertrand T, Bjergarde K, Ma N, Lachaud S, Guizani H, Lebel R, Doerflinger G, Monget S, Perron S, Gasse F, Angouillant-Boniface O, Filoche-Rommé B, Murer M, Gontier S, Prévost C, Monteiro ML, Combeau C. Carry JC, et al. Among authors: schio l. J Med Chem. 2015 Jan 8;58(1):362-75. doi: 10.1021/jm501326k. Epub 2014 Nov 24. J Med Chem. 2015. PMID: 25369539
Corrigendum: An orally available small molecule that targets soluble TNF to deliver anti-TNF biologic-like efficacy in rheumatoid arthritis.
Vugler A, O'connell J, Nguyen MA, Weitz D, Leeuw T, Hickford E, Verbitsky A, Ying X, Rehberg M, Carrington B, Merriman M, Moss A, Nicolas JM, Stanley P, Wright S, Bourne T, Foricher Y, Zhu Z, Brookings D, Horsley H, Heer J, Schio L, Herrmann M, Rao S, Kohlmann M, Florian P. Vugler A, et al. Among authors: schio l. Front Pharmacol. 2024 Oct 16;15:1479557. doi: 10.3389/fphar.2024.1479557. eCollection 2024. Front Pharmacol. 2024. PMID: 39478966 Free PMC article.
Preparation and optimization of new 4-(morpholin-4-yl)-(6-oxo-1,6-dihydropyrimidin-2-yl)amide derivatives as PI3Kβ inhibitors.
Certal V, Halley F, Virone-Oddos A, Thompson F, Filoche-Rommé B, El-Ahmad Y, Carry JC, Delorme C, Karlsson A, Abecassis PY, Vincent L, Bonnevaux H, Nicolas JP, Morales R, Michot N, Vade I, Louboutin A, Perron S, Doerflinger G, Tric B, Monget S, Lengauer C, Schio L. Certal V, et al. Among authors: schio l. Bioorg Med Chem Lett. 2012 Oct 15;22(20):6381-4. doi: 10.1016/j.bmcl.2012.08.072. Epub 2012 Aug 25. Bioorg Med Chem Lett. 2012. PMID: 22981333
Discovery and optimization of pyrimidone indoline amide PI3Kβ inhibitors for the treatment of phosphatase and tensin homologue (PTEN)-deficient cancers.
Certal V, Carry JC, Halley F, Virone-Oddos A, Thompson F, Filoche-Rommé B, El-Ahmad Y, Karlsson A, Charrier V, Delorme C, Rak A, Abecassis PY, Amara C, Vincent L, Bonnevaux H, Nicolas JP, Mathieu M, Bertrand T, Marquette JP, Michot N, Benard T, Perrin MA, Lemaitre O, Guerif S, Perron S, Monget S, Gruss-Leleu F, Doerflinger G, Guizani H, Brollo M, Delbarre L, Bertin L, Richepin P, Loyau V, Garcia-Echeverria C, Lengauer C, Schio L. Certal V, et al. Among authors: schio l. J Med Chem. 2014 Feb 13;57(3):903-20. doi: 10.1021/jm401642q. Epub 2014 Jan 15. J Med Chem. 2014. PMID: 24387221
Preparation and optimization of new 4-(2-(indolin-1-yl)-2-oxoethyl)-2-morpholinothiazole-5-carboxylic acid and amide derivatives as potent and selective PI3Kβ inhibitors.
Certal V, Halley F, Virone-Oddos A, Filoche-Rommé B, Carry JC, Gruss-Leleu F, Bertin L, Guizani H, Pilorge F, Richepin P, Karlsson A, Charrier V, Abecassis PY, Vincent L, Nicolas JP, Lengauer C, Garcia-Echeverria C, Schio L. Certal V, et al. Among authors: schio l. Bioorg Med Chem Lett. 2014 Mar 15;24(6):1506-10. doi: 10.1016/j.bmcl.2014.02.004. Epub 2014 Feb 8. Bioorg Med Chem Lett. 2014. PMID: 24560540
A highly potent and selective Vps34 inhibitor alters vesicle trafficking and autophagy.
Ronan B, Flamand O, Vescovi L, Dureuil C, Durand L, Fassy F, Bachelot MF, Lamberton A, Mathieu M, Bertrand T, Marquette JP, El-Ahmad Y, Filoche-Romme B, Schio L, Garcia-Echeverria C, Goulaouic H, Pasquier B. Ronan B, et al. Among authors: schio l. Nat Chem Biol. 2014 Dec;10(12):1013-9. doi: 10.1038/nchembio.1681. Epub 2014 Oct 19. Nat Chem Biol. 2014. PMID: 25326666
Discovery of (2S)-8-[(3R)-3-methylmorpholin-4-yl]-1-(3-methyl-2-oxobutyl)-2-(trifluoromethyl)-3,4-dihydro-2H-pyrimido[1,2-a]pyrimidin-6-one: a novel potent and selective inhibitor of Vps34 for the treatment of solid tumors.
Pasquier B, El-Ahmad Y, Filoche-Rommé B, Dureuil C, Fassy F, Abecassis PY, Mathieu M, Bertrand T, Benard T, Barrière C, El Batti S, Letallec JP, Sonnefraud V, Brollo M, Delbarre L, Loyau V, Pilorge F, Bertin L, Richepin P, Arigon J, Labrosse JR, Clément J, Durand F, Combet R, Perraut P, Leroy V, Gay F, Lefrançois D, Bretin F, Marquette JP, Michot N, Caron A, Castell C, Schio L, McCort G, Goulaouic H, Garcia-Echeverria C, Ronan B. Pasquier B, et al. Among authors: schio l. J Med Chem. 2015 Jan 8;58(1):376-400. doi: 10.1021/jm5013352. Epub 2014 Nov 26. J Med Chem. 2015. PMID: 25402320
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