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Page 1
Discovery, Synthesis, and Biological Evaluation of Thiazoloquin(az)olin(on)es as Potent CD38 Inhibitors.
Haffner CD, Becherer JD, Boros EE, Cadilla R, Carpenter T, Cowan D, Deaton DN, Guo Y, Harrington W, Henke BR, Jeune MR, Kaldor I, Milliken N, Petrov KG, Preugschat F, Schulte C, Shearer BG, Shearer T, Smalley TL Jr, Stewart EL, Stuart JD, Ulrich JC. Haffner CD, et al. Among authors: petrov kg. J Med Chem. 2015 Apr 23;58(8):3548-71. doi: 10.1021/jm502009h. Epub 2015 Apr 10. J Med Chem. 2015. PMID: 25828863
A knowledge-based, structural-aided discovery of a novel class of 2-phenylimidazo[1,2-a]pyridine-6-carboxamide H-PGDS inhibitors.
Schulte CA, Deaton DN, Diaz E, Do Y, Gampe RT, Guss JH, Hancock AP, Hobbs H, Hodgson ST, Holt J, Jeune MR, Kahler KM, Kramer HF, Le J, Mortenson PN, Musetti C, Nolte RT, Orband-Miller LA, Peckham GE, Petrov KG, Pietrak BL, Poole C, Price DJ, Saxty G, Shillings A, Smalley TL Jr, Somers DO, Stewart EL, Stuart JD, Thomson SA. Schulte CA, et al. Among authors: petrov kg. Bioorg Med Chem Lett. 2021 Sep 1;47:128113. doi: 10.1016/j.bmcl.2021.128113. Epub 2021 May 13. Bioorg Med Chem Lett. 2021. PMID: 33991628
Discovery of Dabrafenib: A Selective Inhibitor of Raf Kinases with Antitumor Activity against B-Raf-Driven Tumors.
Rheault TR, Stellwagen JC, Adjabeng GM, Hornberger KR, Petrov KG, Waterson AG, Dickerson SH, Mook RA Jr, Laquerre SG, King AJ, Rossanese OW, Arnone MR, Smitheman KN, Kane-Carson LS, Han C, Moorthy GS, Moss KG, Uehling DE. Rheault TR, et al. Among authors: petrov kg. ACS Med Chem Lett. 2013 Feb 7;4(3):358-62. doi: 10.1021/ml4000063. eCollection 2013 Mar 14. ACS Med Chem Lett. 2013. PMID: 24900673 Free PMC article.
Development of potent B-RafV600E inhibitors containing an arylsulfonamide headgroup.
Stellwagen JC, Adjabeng GM, Arnone MR, Dickerson SH, Han C, Hornberger KR, King AJ, Mook RA Jr, Petrov KG, Rheault TR, Rominger CM, Rossanese OW, Smitheman KN, Waterson AG, Uehling DE. Stellwagen JC, et al. Among authors: petrov kg. Bioorg Med Chem Lett. 2011 Aug 1;21(15):4436-40. doi: 10.1016/j.bmcl.2011.06.021. Epub 2011 Jun 16. Bioorg Med Chem Lett. 2011. PMID: 21733693
Synthesis and evaluation of aniline headgroups for alkynyl thienopyrimidine dual EGFR/ErbB-2 kinase inhibitors.
Waterson AG, Petrov KG, Hornberger KR, Hubbard RD, Sammond DM, Smith SC, Dickson HD, Caferro TR, Hinkle KW, Stevens KL, Dickerson SH, Rusnak DW, Spehar GM, Wood ER, Griffin RJ, Uehling DE. Waterson AG, et al. Among authors: petrov kg. Bioorg Med Chem Lett. 2009 Mar 1;19(5):1332-6. doi: 10.1016/j.bmcl.2009.01.080. Epub 2009 Feb 7. Bioorg Med Chem Lett. 2009. PMID: 19208477
Thienopyrimidine-based dual EGFR/ErbB-2 inhibitors.
Rheault TR, Caferro TR, Dickerson SH, Donaldson KH, Gaul MD, Goetz AS, Mullin RJ, McDonald OB, Petrov KG, Rusnak DW, Shewchuk LM, Spehar GM, Truesdale AT, Vanderwall DE, Wood ER, Uehling DE. Rheault TR, et al. Among authors: petrov kg. Bioorg Med Chem Lett. 2009 Feb 1;19(3):817-20. doi: 10.1016/j.bmcl.2008.12.011. Epub 2008 Dec 7. Bioorg Med Chem Lett. 2009. PMID: 19111461
Synthesis and stereochemical effects of pyrrolidinyl-acetylenic thieno[3,2-d]pyrimidines as EGFR and ErbB-2 inhibitors.
Stevens KL, Alligood KJ, Alberti JG, Caferro TR, Chamberlain SD, Dickerson SH, Dickson HD, Emerson HK, Griffin RJ, Hubbard RD, Keith BR, Mullin RJ, Petrov KG, Gerding RM, Reno MJ, Rheault TR, Rusnak DW, Sammond DM, Smith SC, Uehling DE, Waterson AG, Wood ER. Stevens KL, et al. Among authors: petrov kg. Bioorg Med Chem Lett. 2009 Jan 1;19(1):21-6. doi: 10.1016/j.bmcl.2008.11.023. Epub 2008 Nov 13. Bioorg Med Chem Lett. 2009. PMID: 19028424
6-Ethynylthieno[3,2-d]- and 6-ethynylthieno[2,3-d]pyrimidin-4-anilines as tunable covalent modifiers of ErbB kinases.
Wood ER, Shewchuk LM, Ellis B, Brignola P, Brashear RL, Caferro TR, Dickerson SH, Dickson HD, Donaldson KH, Gaul M, Griffin RJ, Hassell AM, Keith B, Mullin R, Petrov KG, Reno MJ, Rusnak DW, Tadepalli SM, Ulrich JC, Wagner CD, Vanderwall DE, Waterson AG, Williams JD, White WL, Uehling DE. Wood ER, et al. Among authors: petrov kg. Proc Natl Acad Sci U S A. 2008 Feb 26;105(8):2773-8. doi: 10.1073/pnas.0708281105. Epub 2008 Feb 19. Proc Natl Acad Sci U S A. 2008. PMID: 18287036 Free PMC article.
Substrate specificity and novel selective inhibitors of TNF-alpha converting enzyme (TACE) from two-dimensional substrate mapping.
Lambert MH, Blackburn RK, Seaton TD, Kassel DB, Kinder DS, Leesnitzer MA, Bickett DM, Warner JR, Andersen MW, Badiang JG, Cowan DJ, Gaul MD, Petrov KG, Rabinowitz MH, Wiethe RW, Becherer JD, McDougald DL, Musso DL, Andrews RC, Moss ML. Lambert MH, et al. Among authors: petrov kg. Comb Chem High Throughput Screen. 2005 Jun;8(4):327-39. doi: 10.2174/1386207054020840. Comb Chem High Throughput Screen. 2005. PMID: 16101009
11 results