Howard Bregman - Publications

Affiliations: 
2003-2007 University of Pennsylvania, Philadelphia, PA, United States 

19 high-probability publications. We are testing a new system for linking publications to authors. You can help! If you notice any inaccuracies, please sign in and mark papers as correct or incorrect matches. If you identify any major omissions or other inaccuracies in the publication list, please let us know.

Year Citation  Score
2017 Weiss MM, Dineen TA, Marx IE, Altmann S, Boezio AA, Bregman H, Chu-Moyer MY, DiMauro EF, Feric Bojic E, Foti RS, Gao H, Graceffa RF, Gunaydin H, Guzman-Perez A, Huang H, et al. Sulfonamides as Selective NaV1.7 Inhibitors: Optimizing Potency and Pharmacokinetics While Mitigating Metabolic Liabilities. Journal of Medicinal Chemistry. PMID 28287723 DOI: 10.1021/Acs.Jmedchem.6B01851  0.307
2013 Huang H, Guzman-Perez A, Acquaviva L, Berry V, Bregman H, Dovey J, Gunaydin H, Huang X, Huang L, Saffran D, Serafino R, Schneider S, Wilson C, DiMauro EF. Structure-based design of 2-aminopyridine oxazolidinones as potent and selective tankyrase inhibitors. Acs Medicinal Chemistry Letters. 4: 1218-23. PMID 24900633 DOI: 10.1021/Ml4003315  0.342
2013 Hua Z, Bregman H, Buchanan JL, Chakka N, Guzman-Perez A, Gunaydin H, Huang X, Gu Y, Berry V, Liu J, Teffera Y, Huang L, Egge B, Emkey R, Mullady EL, et al. Development of novel dual binders as potent, selective, and orally bioavailable tankyrase inhibitors. Journal of Medicinal Chemistry. 56: 10003-15. PMID 24294969 DOI: 10.1021/Jm401317Z  0.37
2013 Bregman H, Chakka N, Guzman-Perez A, Gunaydin H, Gu Y, Huang X, Berry V, Liu J, Teffera Y, Huang L, Egge B, Mullady EL, Schneider S, Andrews PS, Mishra A, et al. Discovery of novel, induced-pocket binding oxazolidinones as potent, selective, and orally bioavailable tankyrase inhibitors. Journal of Medicinal Chemistry. 56: 4320-42. PMID 23701517 DOI: 10.1021/Jm4000038  0.397
2013 Bregman H, Gunaydin H, Gu Y, Schneider S, Wilson C, DiMauro EF, Huang X. Discovery of a class of novel tankyrase inhibitors that bind to both the nicotinamide pocket and the induced pocket. Journal of Medicinal Chemistry. 56: 1341-5. PMID 23316926 DOI: 10.1021/Jm301607V  0.397
2012 Huang H, Acquaviva L, Berry V, Bregman H, Chakka N, O'Connor A, DiMauro EF, Dovey J, Epstein O, Grubinska B, Goldstein J, Gunaydin H, Hua Z, Huang X, Huang L, et al. Structure-Based Design of Potent and Selective CK1γ Inhibitors. Acs Medicinal Chemistry Letters. 3: 1059-64. PMID 24900428 DOI: 10.1021/Ml300278F  0.364
2012 Hua Z, Huang X, Bregman H, Chakka N, DiMauro EF, Doherty EM, Goldstein J, Gunaydin H, Huang H, Mercede S, Newcomb J, Patel VF, Turci SM, Yan J, Wilson C, et al. 2-Phenylamino-6-cyano-1H-benzimidazole-based isoform selective casein kinase 1 gamma (CK1γ) inhibitors. Bioorganic & Medicinal Chemistry Letters. 22: 5392-5. PMID 22877629 DOI: 10.1016/J.Bmcl.2012.07.046  0.462
2009 Pagano N, Wong EY, Breiding T, Liu H, Wilbuer A, Bregman H, Shen Q, Diamond SL, Meggers E. From imide to lactam metallo-pyridocarbazoles: distinct scaffolds for the design of selective protein kinase inhibitors. The Journal of Organic Chemistry. 74: 8997-9009. PMID 19886617 DOI: 10.1021/Jo901641K  0.796
2009 Bullock AN, Russo S, Amos A, Pagano N, Bregman H, Debreczeni JE, Lee WH, von Delft F, Meggers E, Knapp S. Crystal structure of the PIM2 kinase in complex with an organoruthenium inhibitor. Plos One. 4: e7112. PMID 19841674 DOI: 10.1371/Journal.Pone.0007112  0.752
2009 Xie P, Streu C, Qin J, Bregman H, Pagano N, Meggers E, Marmorstein R. The crystal structure of BRAF in complex with an organoruthenium inhibitor reveals a mechanism for inhibition of an active form of BRAF kinase. Biochemistry. 48: 5187-98. PMID 19371126 DOI: 10.1021/Bi802067U  0.789
2007 Pagano N, Maksimoska J, Bregman H, Williams DS, Webster RD, Xue F, Meggers E. Ruthenium half-sandwich complexes as protein kinase inhibitors: derivatization of the pyridocarbazole pharmacophore ligand. Organic & Biomolecular Chemistry. 5: 1218-27. PMID 17406720 DOI: 10.1039/B700433H  0.746
2007 Smalley KS, Contractor R, Haass NK, Kulp AN, Atilla-Gokcumen GE, Williams DS, Bregman H, Flaherty KT, Soengas MS, Meggers E, Herlyn M. An organometallic protein kinase inhibitor pharmacologically activates p53 and induces apoptosis in human melanoma cells. Cancer Research. 67: 209-17. PMID 17210701 DOI: 10.1158/0008-5472.Can-06-1538  0.709
2006 Bregman H, Meggers E. Ruthenium half-sandwich complexes as protein kinase inhibitors: an N-succinimidyl ester for rapid derivatizations of the cyclopentadienyl moiety. Organic Letters. 8: 5465-8. PMID 17107048 DOI: 10.1021/Ol0620646  0.745
2006 Atilla-Gokcumen GE, Williams DS, Bregman H, Pagano N, Meggers E. Organometallic compounds with biological activity: a very selective and highly potent cellular inhibitor for glycogen synthase kinase 3. Chembiochem : a European Journal of Chemical Biology. 7: 1443-50. PMID 16858717 DOI: 10.1002/Cbic.200600117  0.751
2006 Bregman H, Carroll PJ, Meggers E. Rapid access to unexplored chemical space by ligand scanning around a ruthenium center: discovery of potent and selective protein kinase inhibitors. Journal of the American Chemical Society. 128: 877-84. PMID 16417378 DOI: 10.1021/Ja055523R  0.741
2006 Debreczeni JE, Bullock AN, Atilla GE, Williams DS, Bregman H, Knapp S, Meggers E. Ruthenium half-sandwich complexes bound to protein kinase Pim-1. Angewandte Chemie (International Ed. in English). 45: 1580-5. PMID 16381041 DOI: 10.1002/Anie.200503468  0.806
2006 Debreczeni JÉ, Bullock AN, Atilla GE, Williams DS, Bregman H, Knapp S, Meggers E. Ruthenium Half-Sandwich Complexes Bound to Protein Kinase Pim-1 Angewandte Chemie. 118: 1610-1615. DOI: 10.1002/ange.200503468  0.806
2005 Williams DS, Atilla GE, Bregman H, Arzoumanian A, Klein PS, Meggers E. Switching on a signaling pathway with an organoruthenium complex. Angewandte Chemie (International Ed. in English). 44: 1984-7. PMID 15742314 DOI: 10.1002/Anie.200462501  0.781
2004 Bregman H, Williams DS, Atilla GE, Carroll PJ, Meggers E. An organometallic inhibitor for glycogen synthase kinase 3. Journal of the American Chemical Society. 126: 13594-5. PMID 15493898 DOI: 10.1021/Ja046049C  0.81
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