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209 results

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Page 1
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: delorme c. 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 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: delorme c. J Med Chem. 2012 May 24;55(10):4788-805. doi: 10.1021/jm300241b. Epub 2012 May 2. J Med Chem. 2012. PMID: 22524426
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: delorme c. J Med Chem. 2014 Feb 13;57(3):903-20. doi: 10.1021/jm401642q. Epub 2014 Jan 15. J Med Chem. 2014. PMID: 24387221
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: delorme c. J Med Chem. 2015 Jan 8;58(1):362-75. doi: 10.1021/jm501326k. Epub 2014 Nov 24. J Med Chem. 2015. PMID: 25369539
Concomitant Inhibition of PI3Kβ and BRAF or MEK in PTEN-Deficient/BRAF-Mutant Melanoma Treatment: Preclinical Assessment of SAR260301 Oral PI3Kβ-Selective Inhibitor.
Bonnevaux H, Lemaitre O, Vincent L, Levit MN, Windenberger F, Halley F, Delorme C, Lengauer C, Garcia-Echeverria C, Virone-Oddos A. Bonnevaux H, et al. Among authors: delorme c. Mol Cancer Ther. 2016 Jul;15(7):1460-71. doi: 10.1158/1535-7163.MCT-15-0496. Epub 2016 May 12. Mol Cancer Ther. 2016. PMID: 27196754
Tricyclic series of heat shock protein 90 (Hsp90) inhibitors part I: discovery of tricyclic imidazo[4,5-c]pyridines as potent inhibitors of the Hsp90 molecular chaperone.
Vallée F, Carrez C, Pilorge F, Dupuy A, Parent A, Bertin L, Thompson F, Ferrari P, Fassy F, Lamberton A, Thomas A, Arrebola R, Guerif S, Rohaut A, Certal V, Ruxer JM, Gouyon T, Delorme C, Jouanen A, Dumas J, Grépin C, Combeau C, Goulaouic H, Dereu N, Mikol V, Mailliet P, Minoux H. Vallée F, et al. Among authors: delorme c. J Med Chem. 2011 Oct 27;54(20):7206-19. doi: 10.1021/jm200784m. Epub 2011 Oct 5. J Med Chem. 2011. PMID: 21972823
The use of virtual screening and differential scanning fluorimetry for the rapid identification of fragments active against MEK1.
Amaning K, Lowinski M, Vallee F, Steier V, Marcireau C, Ugolini A, Delorme C, Foucalt F, McCort G, Derimay N, Andouche C, Vougier S, Llopart S, Halland N, Rak A. Amaning K, et al. Among authors: delorme c. Bioorg Med Chem Lett. 2013 Jun 15;23(12):3620-6. doi: 10.1016/j.bmcl.2013.04.003. Epub 2013 Apr 10. Bioorg Med Chem Lett. 2013. PMID: 23648182
18-Vinyldeoxycorticosterone: a potent inhibitor of the bovine cytochrome P-450(11) beta.
Davioud E, Piffeteau A, Delorme C, Coustal S, Marquet A. Davioud E, et al. Among authors: delorme c. Bioorg Med Chem. 1998 Oct;6(10):1781-8. doi: 10.1016/s0968-0896(98)00106-0. Bioorg Med Chem. 1998. PMID: 9839008
18-Vinylprogesterone (18-VP) and 18-ethynylprogesterone (18-EP) have proved to be potent suicide inhibitors of P-450(11) beta, the last enzyme of aldosterone biosynthesis (Delorme, C.; Piffeteau, A.; Viger, A.; Marquet, A. Eur. J. Biochem. 1995, 232, 247; Delorme …
18-Vinylprogesterone (18-VP) and 18-ethynylprogesterone (18-EP) have proved to be potent suicide inhibitors of P-450(11) beta, the last enzy …
KRAS G12C fragment screening renders new binding pockets.
Mathieu M, Steier V, Fassy F, Delorme C, Papin D, Genet B, Duffieux F, Bertrand T, Delarbre L, Le-Borgne H, Parent A, Didier P, Marquette JP, Lowinski M, Houtmann J, Lamberton A, Debussche L, Alexey R. Mathieu M, et al. Among authors: delorme c. Small GTPases. 2022 Jan;13(1):225-238. doi: 10.1080/21541248.2021.1979360. Epub 2021 Sep 24. Small GTPases. 2022. PMID: 34558391 Free PMC article.
209 results