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Pyridoimidazolones as novel potent inhibitors of v-Raf murine sarcoma viral oncogene homologue B1 (BRAF).
Niculescu-Duvaz D, Gaulon C, Dijkstra HP, Niculescu-Duvaz I, Zambon A, Ménard D, Suijkerbuijk BM, Nourry A, Davies L, Manne H, Friedlos F, Ogilvie L, Hedley D, Whittaker S, Kirk R, Gill A, Taylor RD, Raynaud FI, Moreno-Farre J, Marais R, Springer CJ. Niculescu-Duvaz D, et al. Among authors: kirk r. J Med Chem. 2009 Apr 23;52(8):2255-64. doi: 10.1021/jm801509w. J Med Chem. 2009. PMID: 19323560
Development of novel, highly potent inhibitors of V-RAF murine sarcoma viral oncogene homologue B1 (BRAF): increasing cellular potency through optimization of a distal heteroaromatic group.
Suijkerbuijk BM, Niculescu-Duvaz I, Gaulon C, Dijkstra HP, Niculescu-Duvaz D, Ménard D, Zambon A, Nourry A, Davies L, Manne HA, Friedlos F, Ogilvie LM, Hedley D, Lopes F, Preece NP, Moreno-Farre J, Raynaud FI, Kirk R, Whittaker S, Marais R, Springer CJ. Suijkerbuijk BM, et al. Among authors: kirk r. J Med Chem. 2010 Apr 8;53(7):2741-56. doi: 10.1021/jm900607f. J Med Chem. 2010. PMID: 20199087
Gatekeeper mutations mediate resistance to BRAF-targeted therapies.
Whittaker S, Kirk R, Hayward R, Zambon A, Viros A, Cantarino N, Affolter A, Nourry A, Niculescu-Duvaz D, Springer C, Marais R. Whittaker S, et al. Among authors: kirk r. Sci Transl Med. 2010 Jun 9;2(35):35ra41. doi: 10.1126/scitranslmed.3000758. Sci Transl Med. 2010. PMID: 20538618
Novel hinge binder improves activity and pharmacokinetic properties of BRAF inhibitors.
Zambon A, Ménard D, Suijkerbuijk BM, Niculescu-Duvaz I, Whittaker S, Niculescu-Duvaz D, Nourry A, Davies L, Manne HA, Lopes F, Preece N, Hedley D, Ogilvie LM, Kirk R, Marais R, Springer CJ. Zambon A, et al. Among authors: kirk r. J Med Chem. 2010 Aug 12;53(15):5639-55. doi: 10.1021/jm100383b. J Med Chem. 2010. PMID: 20597484
Novel tricyclic pyrazole BRAF inhibitors with imidazole or furan central scaffolds.
Niculescu-Duvaz D, Niculescu-Duvaz I, Suijkerbuijk BM, Ménard D, Zambon A, Nourry A, Davies L, Manne HA, Friedlos F, Ogilvie L, Hedley D, Takle AK, Wilson DM, Pons JF, Coulter T, Kirk R, Cantarino N, Whittaker S, Marais R, Springer CJ. Niculescu-Duvaz D, et al. Among authors: kirk r. Bioorg Med Chem. 2010 Sep 15;18(18):6934-52. doi: 10.1016/j.bmc.2010.06.031. Epub 2010 Jun 15. Bioorg Med Chem. 2010. PMID: 20667740 Free PMC article.
1,011 results