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Influence of acid surrogates toward potency of VLA-4 antagonist.
Venkatraman S, Lim J, Cramer M, Gardner MF, James J, Alves K, Lingham RB, Mumford RA, Munoz B. Venkatraman S, et al. Among authors: cramer m. Bioorg Med Chem Lett. 2005 Sep 15;15(18):4053-6. doi: 10.1016/j.bmcl.2005.06.034. Bioorg Med Chem Lett. 2005. PMID: 16039122
Identification of N-(5-tert-butyl-isoxazol-3-yl)-N'-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,1-b][1,3]benzothiazol-2-yl]phenyl}urea dihydrochloride (AC220), a uniquely potent, selective, and efficacious FMS-like tyrosine kinase-3 (FLT3) inhibitor.
Chao Q, Sprankle KG, Grotzfeld RM, Lai AG, Carter TA, Velasco AM, Gunawardane RN, Cramer MD, Gardner MF, James J, Zarrinkar PP, Patel HK, Bhagwat SS. Chao Q, et al. Among authors: cramer md. J Med Chem. 2009 Dec 10;52(23):7808-16. doi: 10.1021/jm9007533. J Med Chem. 2009. PMID: 19754199
4-Quinazolinyloxy-diaryl ureas as novel BRAFV600E inhibitors.
Holladay MW, Campbell BT, Rowbottom MW, Chao Q, Sprankle KG, Lai AG, Abraham S, Setti E, Faraoni R, Tran L, Armstrong RC, Gunawardane RN, Gardner MF, Cramer MD, Gitnick D, Ator MA, Dorsey BD, Ruggeri BR, Williams M, Bhagwat SS, James J. Holladay MW, et al. Among authors: cramer md. Bioorg Med Chem Lett. 2011 Sep 15;21(18):5342-6. doi: 10.1016/j.bmcl.2011.07.019. Epub 2011 Jul 14. Bioorg Med Chem Lett. 2011. PMID: 21807507
Synthesis and biological evaluation of 6-aryl-6H-pyrrolo[3,4-d]pyridazine derivatives: high-affinity ligands to the alpha 2 delta subunit of voltage gated calcium channels.
Stearns BA, Anker N, Arruda JM, Campbell BT, Chen C, Cramer M, Hu T, Jiang X, Park K, Ren KK, Sablad M, Santini A, Schaffhauser H, Urban MO, Munoz B. Stearns BA, et al. Among authors: cramer m. Bioorg Med Chem Lett. 2004 Mar 8;14(5):1295-8. doi: 10.1016/j.bmcl.2003.12.036. Bioorg Med Chem Lett. 2004. PMID: 14980685
5-[(2-Methyl-1,3-thiazol-4-yl)ethynyl]-2,3'-bipyridine: a highly potent, orally active metabotropic glutamate subtype 5 (mGlu5) receptor antagonist with anxiolytic activity.
Roppe JR, Wang B, Huang D, Tehrani L, Kamenecka T, Schweiger EJ, Anderson JJ, Brodkin J, Jiang X, Cramer M, Chung J, Reyes-Manalo G, Munoz B, Cosford ND. Roppe JR, et al. Among authors: cramer m. Bioorg Med Chem Lett. 2004 Aug 2;14(15):3993-6. doi: 10.1016/j.bmcl.2004.05.037. Bioorg Med Chem Lett. 2004. PMID: 15225713
Novel series of pyrrolotriazine analogs as highly potent pan-Aurora kinase inhibitors.
Abraham S, Hadd MJ, Tran L, Vickers T, Sindac J, Milanov ZV, Holladay MW, Bhagwat SS, Hua H, Ford Pulido JM, Cramer MD, Gitnick D, James J, Dao A, Belli B, Armstrong RC, Treiber DK, Liu G. Abraham S, et al. Among authors: cramer md. Bioorg Med Chem Lett. 2011 Sep 15;21(18):5296-300. doi: 10.1016/j.bmcl.2011.07.027. Epub 2011 Jul 14. Bioorg Med Chem Lett. 2011. PMID: 21802948
Identification of 1-(3-(6,7-dimethoxyquinazolin-4-yloxy)phenyl)-3-(5-(1,1,1-trifluoro-2-methylpropan-2-yl)isoxazol-3-yl)urea hydrochloride (CEP-32496), a highly potent and orally efficacious inhibitor of V-RAF murine sarcoma viral oncogene homologue B1 (BRAF) V600E.
Rowbottom MW, Faraoni R, Chao Q, Campbell BT, Lai AG, Setti E, Ezawa M, Sprankle KG, Abraham S, Tran L, Struss B, Gibney M, Armstrong RC, Gunawardane RN, Nepomuceno RR, Valenta I, Hua H, Gardner MF, Cramer MD, Gitnick D, Insko DE, Apuy JL, Jones-Bolin S, Ghose AK, Herbertz T, Ator MA, Dorsey BD, Ruggeri B, Williams M, Bhagwat S, James J, Holladay MW. Rowbottom MW, et al. Among authors: cramer md. J Med Chem. 2012 Feb 9;55(3):1082-105. doi: 10.1021/jm2009925. Epub 2012 Jan 23. J Med Chem. 2012. PMID: 22168626
850 results