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Concise Stereoselective Routes to Advanced Intermediates Related to Natural and Unnatural Pinnaic Acid This work was supported by the National Institutes of Health (Grant Numbers: CA28824). Postdoctoral Fellowship support is gratefully acknowledged by M.W.C. (U.S. Army BCRP, DAMD17-98-1-8154), M.F.H. (5T32 CA62948-05), and D.T. (Schering Research Foundation, Berlin). We thank Dr. George Sukenick of the MSKCC NMR Core Facility for NMR and mass spectral analyses.
Carson MW, Kim G, Hentemann MF, Trauner D, Danishefsky SJ. Carson MW, et al. Angew Chem Int Ed Engl. 2001 Dec 3;40(23):4450-4452. doi: 10.1002/1521-3773(20011203)40:23<4450::aid-anie4450>3.0.co;2-m. Angew Chem Int Ed Engl. 2001. PMID: 12404442 No abstract available.
Indanylacetic acids as PPAR-delta activator insulin sensitizers.
Wickens P, Zhang C, Ma X, Zhao Q, Amatruda J, Bullock W, Burns M, Cantin LD, Chuang CY, Claus T, Dai M, Dela Cruz F, Dickson D, Ehrgott FJ, Fan D, Heald S, Hentemann M, Iwuagwu CI, Johnson JS, Kumarasinghe E, Ladner D, Lavoie R, Liang S, Livingston JN, Lowe D, Magnuson S, Mannelly G, Mugge I, Ogutu H, Pleasic-Williams S, Schoenleber RW, Shapiro J, Shelekhin T, Sweet L, Town C, Tsutsumi M. Wickens P, et al. Among authors: hentemann m. Bioorg Med Chem Lett. 2007 Aug 1;17(15):4369-73. doi: 10.1016/j.bmcl.2007.03.057. Epub 2007 Mar 23. Bioorg Med Chem Lett. 2007. PMID: 17601734
Discovery of selective and potent inhibitors of gram-positive bacterial thymidylate kinase (TMK).
Martínez-Botella G, Breen JN, Duffy JE, Dumas J, Geng B, Gowers IK, Green OM, Guler S, Hentemann MF, Hernandez-Juan FA, Joseph-McCarthy D, Kawatkar S, Larsen NA, Lazari O, Loch JT, Macritchie JA, McKenzie AR, Newman JV, Olivier NB, Otterson LG, Owens AP, Read J, Sheppard DW, Keating TA. Martínez-Botella G, et al. Among authors: hentemann mf. J Med Chem. 2012 Nov 26;55(22):10010-21. doi: 10.1021/jm3011806. Epub 2012 Oct 24. J Med Chem. 2012. PMID: 23043329
Discovery and SAR of Novel 2,3-Dihydroimidazo[1,2-c]quinazoline PI3K Inhibitors: Identification of Copanlisib (BAY 80-6946).
Scott WJ, Hentemann MF, Rowley RB, Bull CO, Jenkins S, Bullion AM, Johnson J, Redman A, Robbins AH, Esler W, Fracasso RP, Garrison T, Hamilton M, Michels M, Wood JE, Wilkie DP, Xiao H, Levy J, Stasik E, Liu N, Schaefer M, Brands M, Lefranc J. Scott WJ, et al. Among authors: hentemann mf. ChemMedChem. 2016 Jul 19;11(14):1517-30. doi: 10.1002/cmdc.201600148. Epub 2016 Jun 16. ChemMedChem. 2016. PMID: 27310202 Free PMC article.
In vivo validation of thymidylate kinase (TMK) with a rationally designed, selective antibacterial compound.
Keating TA, Newman JV, Olivier NB, Otterson LG, Andrews B, Boriack-Sjodin PA, Breen JN, Doig P, Dumas J, Gangl E, Green OM, Guler SY, Hentemann MF, Joseph-McCarthy D, Kawatkar S, Kutschke A, Loch JT, McKenzie AR, Pradeepan S, Prasad S, Martínez-Botella G. Keating TA, et al. Among authors: hentemann mf. ACS Chem Biol. 2012 Nov 16;7(11):1866-72. doi: 10.1021/cb300316n. Epub 2012 Aug 28. ACS Chem Biol. 2012. PMID: 22908966
Antibacterial inhibitors of Gram-positive thymidylate kinase: structure-activity relationships and chiral preference of a new hydrophobic binding region.
Kawatkar SP, Keating TA, Olivier NB, Breen JN, Green OM, Guler SY, Hentemann MF, Loch JT, McKenzie AR, Newman JV, Otterson LG, Martínez-Botella G. Kawatkar SP, et al. Among authors: hentemann mf. J Med Chem. 2014 Jun 12;57(11):4584-97. doi: 10.1021/jm500463c. Epub 2014 Jun 3. J Med Chem. 2014. PMID: 24828090
BAY 80-6946 is a highly selective intravenous PI3K inhibitor with potent p110α and p110δ activities in tumor cell lines and xenograft models.
Liu N, Rowley BR, Bull CO, Schneider C, Haegebarth A, Schatz CA, Fracasso PR, Wilkie DP, Hentemann M, Wilhelm SM, Scott WJ, Mumberg D, Ziegelbauer K. Liu N, et al. Among authors: hentemann m. Mol Cancer Ther. 2013 Nov;12(11):2319-30. doi: 10.1158/1535-7163.MCT-12-0993-T. Epub 2013 Oct 29. Mol Cancer Ther. 2013. PMID: 24170767
28 results