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Page 1
Design of 1-piperazinyl-4-arylphthalazines as potent Smoothened antagonists.
Lucas BS, Aaron W, An S, Austin RJ, Brown M, Chan H, Chong A, Hungate R, Huang T, Jiang B, Johnson MG, Kaizerman JA, Lee G, McMinn DL, Orf J, Powers JP, Rong M, Toteva MM, Uyeda C, Wickramasinghe D, Xu G, Ye Q, Zhong W. Lucas BS, et al. Among authors: kaizerman ja. Bioorg Med Chem Lett. 2010 Jun 15;20(12):3618-22. doi: 10.1016/j.bmcl.2010.04.110. Epub 2010 Apr 28. Bioorg Med Chem Lett. 2010. PMID: 20493695
Synthesis and optimization of novel 4,4-disubstituted cyclohexylbenzamide derivatives as potent 11β-HSD1 inhibitors.
Sun D, Wang Z, Caille S, DeGraffenreid M, Gonzalez-Lopez de Turiso F, Hungate R, Jaen JC, Jiang B, Julian LD, Kelly R, McMinn DL, Kaizerman J, Rew Y, Sudom A, Tu H, Ursu S, Walker N, Willcockson M, Yan X, Ye Q, Powers JP. Sun D, et al. Bioorg Med Chem Lett. 2011 Jan 1;21(1):405-10. doi: 10.1016/j.bmcl.2010.10.129. Epub 2010 Oct 31. Bioorg Med Chem Lett. 2011. PMID: 21093258
Addressing PXR liabilities of phthalazine-based hedgehog/smoothened antagonists using novel pyridopyridazines.
Kaizerman JA, Aaron W, An S, Austin R, Brown M, Chong A, Huang T, Hungate R, Jiang B, Johnson MG, Lee G, Lucas BS, Orf J, Rong M, Toteva MM, Wickramasinghe D, Xu G, Ye Q, Zhong W, McMinn DL. Kaizerman JA, et al. Bioorg Med Chem Lett. 2010 Aug 1;20(15):4607-10. doi: 10.1016/j.bmcl.2010.06.006. Epub 2010 Jun 8. Bioorg Med Chem Lett. 2010. PMID: 20594845
Discovery of amide replacements that improve activity and metabolic stability of a bis-amide smoothened antagonist hit.
Brown ML, Aaron W, Austin RJ, Chong A, Huang T, Jiang B, Kaizerman JA, Lee G, Lucas BS, McMinn DL, Orf J, Rong M, Toteva MM, Xu G, Ye Q, Zhong W, Degraffenreid MR, Wickramasinghe D, Powers JP, Hungate R, Johnson MG. Brown ML, et al. Among authors: kaizerman ja. Bioorg Med Chem Lett. 2011 Sep 15;21(18):5206-9. doi: 10.1016/j.bmcl.2011.07.052. Epub 2011 Jul 23. Bioorg Med Chem Lett. 2011. PMID: 21840217
Discovery of AMG 925, a FLT3 and CDK4 dual kinase inhibitor with preferential affinity for the activated state of FLT3.
Li Z, Wang X, Eksterowicz J, Gribble MW Jr, Alba GQ, Ayres M, Carlson TJ, Chen A, Chen X, Cho R, Connors RV, DeGraffenreid M, Deignan JT, Duquette J, Fan P, Fisher B, Fu J, Huard JN, Kaizerman J, Keegan KS, Li C, Li K, Li Y, Liang L, Liu W, Lively SE, Lo MC, Ma J, McMinn DL, Mihalic JT, Modi K, Ngo R, Pattabiraman K, Piper DE, Queva C, Ragains ML, Suchomel J, Thibault S, Walker N, Wang X, Wang Z, Wanska M, Wehn PM, Weidner MF, Zhang AJ, Zhao X, Kamb A, Wickramasinghe D, Dai K, McGee LR, Medina JC. Li Z, et al. J Med Chem. 2014 Apr 24;57(8):3430-49. doi: 10.1021/jm500118j. Epub 2014 Apr 2. J Med Chem. 2014. PMID: 24641103
An efficient and scalable one-pot double Michael addition-Dieckmann condensation for the synthesis of 4,4-disubstituted cyclohexane beta-keto esters.
DeGraffenreid MR, Bennett S, Caille S, Gonzalez-Lopez de Turiso F, Hungate RW, Julian LD, Kaizerman JA, McMinn DL, Rew Y, Sun D, Yan X, Powers JP. DeGraffenreid MR, et al. Among authors: kaizerman ja. J Org Chem. 2007 Sep 14;72(19):7455-8. doi: 10.1021/jo071202h. Epub 2007 Aug 14. J Org Chem. 2007. PMID: 17696402
15 results