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Fragment-Based Discovery of 7-Azabenzimidazoles as Potent, Highly Selective, and Orally Active CDK4/6 Inhibitors.
Cho YS, Angove H, Brain C, Chen CH, Cheng H, Cheng R, Chopra R, Chung K, Congreve M, Dagostin C, Davis DJ, Feltell R, Giraldes J, Hiscock SD, Kim S, Kovats S, Lagu B, Lewry K, Loo A, Lu Y, Luzzio M, Maniara W, McMenamin R, Mortenson PN, Benning R, O'Reilly M, Rees DC, Shen J, Smith T, Wang Y, Williams G, Woolford AJ, Wrona W, Xu M, Yang F, Howard S. Cho YS, et al. Among authors: brain c. ACS Med Chem Lett. 2012 May 17;3(6):445-9. doi: 10.1021/ml200241a. eCollection 2012 Jun 14. ACS Med Chem Lett. 2012. PMID: 24900493 Free PMC article.
4-(Pyrazol-4-yl)-pyrimidines as selective inhibitors of cyclin-dependent kinase 4/6.
Cho YS, Borland M, Brain C, Chen CH, Cheng H, Chopra R, Chung K, Groarke J, He G, Hou Y, Kim S, Kovats S, Lu Y, O'Reilly M, Shen J, Smith T, Trakshel G, Vögtle M, Xu M, Xu M, Sung MJ. Cho YS, et al. Among authors: brain c. J Med Chem. 2010 Nov 25;53(22):7938-57. doi: 10.1021/jm100571n. Epub 2010 Nov 1. J Med Chem. 2010. PMID: 21038853
The potent and selective cyclin-dependent kinases 4 and 6 inhibitor ribociclib (LEE011) is a versatile combination partner in preclinical cancer models.
Kim S, Tiedt R, Loo A, Horn T, Delach S, Kovats S, Haas K, Engstler BS, Cao A, Pinzon-Ortiz M, Mulford I, Acker MG, Chopra R, Brain C, di Tomaso E, Sellers WR, Caponigro G. Kim S, et al. Among authors: brain c. Oncotarget. 2018 Oct 16;9(81):35226-35240. doi: 10.18632/oncotarget.26215. eCollection 2018 Oct 16. Oncotarget. 2018. PMID: 30443290 Free PMC article.
Correction: The potent and selective cyclin-dependent kinases 4 and 6 inhibitor ribociclib (LEE011) is a versatile combination partner in preclinical cancer models.
Kim S, Tiedt R, Loo A, Horn T, Delach S, Kovats S, Haas K, Engstler BS, Cao A, Pinzon-Ortiz M, Mulford I, Acker MG, Chopra R, Brain C, Tomaso ED, Sellers WR, Caponigro G. Kim S, et al. Among authors: brain c. Oncotarget. 2020 Apr 7;11(14):1289. doi: 10.18632/oncotarget.27407. eCollection 2020 Apr 7. Oncotarget. 2020. PMID: 32292577 Free PMC article.
Naphthalen-1-yl-(4-pentyloxynaphthalen-1-yl)methanone: a potent, orally bioavailable human CB1/CB2 dual agonist with antihyperalgesic properties and restricted central nervous system penetration.
Dziadulewicz EK, Bevan SJ, Brain CT, Coote PR, Culshaw AJ, Davis AJ, Edwards LJ, Fisher AJ, Fox AJ, Gentry C, Groarke A, Hart TW, Huber W, James IF, Kesingland A, La Vecchia L, Loong Y, Lyothier I, McNair K, O'Farrell C, Peacock M, Portmann R, Schopfer U, Yaqoob M, Zadrobilek J. Dziadulewicz EK, et al. Among authors: brain ct. J Med Chem. 2007 Aug 9;50(16):3851-6. doi: 10.1021/jm070317a. Epub 2007 Jul 14. J Med Chem. 2007. PMID: 17630726
Increased lysosomal biomass is responsible for the resistance of triple-negative breast cancers to CDK4/6 inhibition.
Fassl A, Brain C, Abu-Remaileh M, Stukan I, Butter D, Stepien P, Feit AS, Bergholz J, Michowski W, Otto T, Sheng Q, Loo A, Michael W, Tiedt R, DeAngelis C, Schiff R, Jiang B, Jovanovic B, Nowak K, Ericsson M, Cameron M, Gray N, Dillon D, Zhao JJ, Sabatini DM, Jeselsohn R, Brown M, Polyak K, Sicinski P. Fassl A, et al. Among authors: brain c. Sci Adv. 2020 Jun 17;6(25):eabb2210. doi: 10.1126/sciadv.abb2210. eCollection 2020 Jun. Sci Adv. 2020. PMID: 32704543 Free PMC article.
Sulfonamido-aryl ethers as bradykinin B1 receptor antagonists.
Cole AG, Metzger A, Brescia MR, Qin LY, Appell KC, Brain CT, Hallett A, Ganju P, Denholm AA, Wareing JR, Ritchie TJ, Drake GM, Bevan SJ, MacGloinn A, McBryde A, Patel V, Oakley PJ, Nunez X, Gstach H, Schneider P, Baldwin JJ, Dolle RE, McDonald E, Henderson I. Cole AG, et al. Among authors: brain ct. Bioorg Med Chem Lett. 2009 Jan 1;19(1):119-22. doi: 10.1016/j.bmcl.2008.11.005. Epub 2008 Nov 6. Bioorg Med Chem Lett. 2009. PMID: 19014884
139 results