Howard Bregman - Publications

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

20 high-probability publications. We are testing a new system for linking publications to authors. You can help! If you notice any innacuracies, 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
2016 DiMauro EF, Altmann S, Berry LM, Bregman H, Chakka N, Chu-Moyer M, Feric Bojic E, Foti RS, Fremeau RT, Gao H, Gunaydin H, Guzman-Perez A, Hall BE, Huang H, Jarosh M, et al. Application of a Parallel Synthetic Strategy in the Discovery of Biaryl Acyl Sulfonamides as Efficient and Selective NaV1.7 Inhibitors. Journal of Medicinal Chemistry. PMID 27441383 DOI: 10.1021/acs.jmedchem.6b00425  0.52
2016 Liu L, Lee MR, Kim JL, Whittington DA, Bregman H, Hua Z, Lewis RT, Martin MW, Nishimura N, Potashman M, Yang K, Yi S, Vaida KR, Epstein LF, Babij C, et al. Purinylpyridinylamino-based DFG-in/αC-helix-out B-Raf inhibitors: Applying mutant versus wild-type B-Raf selectivity indices for compound profiling. Bioorganic & Medicinal Chemistry. PMID 27085672 DOI: 10.1016/j.bmc.2016.03.055  0.52
2015 Matson DJ, Hamamoto DT, Bregman H, Cooke M, DiMauro EF, Huang L, Johnson D, Li X, McDermott J, Morgan C, Wilenkin B, Malmberg AB, McDonough SI, Simone DA. Inhibition of Inactive States of Tetrodotoxin-Sensitive Sodium Channels Reduces Spontaneous Firing of C-Fiber Nociceptors and Produces Analgesia in Formalin and Complete Freund's Adjuvant Models of Pain. Plos One. 10: e0138140. PMID 26379236 DOI: 10.1371/journal.pone.0138140  0.52
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  0.52
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  0.52
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  0.52
2012 Bregman H, Nguyen HN, Feric E, Ligutti J, Liu D, McDermott JS, Wilenkin B, Zou A, Huang L, Li X, McDonough SI, Dimauro EF. The discovery of aminopyrazines as novel, potent Na(v)1.7 antagonists: hit-to-lead identification and SAR. Bioorganic & Medicinal Chemistry Letters. 22: 2033-42. PMID 22306122 DOI: 10.1016/j.bmcl.2012.01.023  0.52
2011 Bregman H, Berry L, Buchanan JL, Chen A, Du B, Feric E, Hierl M, Huang L, Immke D, Janosky B, Johnson D, Li X, Ligutti J, Liu D, Malmberg A, et al. Identification of a potent, state-dependent inhibitor of Nav1.7 with oral efficacy in the formalin model of persistent pain. Journal of Medicinal Chemistry. 54: 4427-45. PMID 21634377 DOI: 10.1021/jm200018k  0.52
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  0.52
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  0.52
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  0.52
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  0.52
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  0.52
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  0.52
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  0.52
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  0.52
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  0.52
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  0.52
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  0.52
2004 Handy ST, Zhang Y, Bregman H. A modular synthesis of the lamellarins: total synthesis of lamellarin G trimethyl ether. The Journal of Organic Chemistry. 69: 2362-6. PMID 15049631 DOI: 10.1021/jo0352833  0.52
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