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Discovery of Clinical Candidate 1-{[(2S,3S,4S)-3-Ethyl-4-fluoro-5-oxopyrrolidin-2-yl]methoxy}-7-methoxyisoquinoline-6-carboxamide (PF-06650833), a Potent, Selective Inhibitor of Interleukin-1 Receptor Associated Kinase 4 (IRAK4), by Fragment-Based Drug Design.
Lee KL, Ambler CM, Anderson DR, Boscoe BP, Bree AG, Brodfuehrer JI, Chang JS, Choi C, Chung S, Curran KJ, Day JE, Dehnhardt CM, Dower K, Drozda SE, Frisbie RK, Gavrin LK, Goldberg JA, Han S, Hegen M, Hepworth D, Hope HR, Kamtekar S, Kilty IC, Lee A, Lin LL, Lovering FE, Lowe MD, Mathias JP, Morgan HM, Murphy EA, Papaioannou N, Patny A, Pierce BS, Rao VR, Saiah E, Samardjiev IJ, Samas BM, Shen MWH, Shin JH, Soutter HH, Strohbach JW, Symanowicz PT, Thomason JR, Trzupek JD, Vargas R, Vincent F, Yan J, Zapf CW, Wright SW. Lee KL, et al. Among authors: samas bm. J Med Chem. 2017 Jul 13;60(13):5521-5542. doi: 10.1021/acs.jmedchem.7b00231. Epub 2017 Jun 14. J Med Chem. 2017. PMID: 28498658
Identification of a Chemical Probe for Family VIII Bromodomains through Optimization of a Fragment Hit.
Gerstenberger BS, Trzupek JD, Tallant C, Fedorov O, Filippakopoulos P, Brennan PE, Fedele V, Martin S, Picaud S, Rogers C, Parikh M, Taylor A, Samas B, O'Mahony A, Berg E, Pallares G, Torrey AD, Treiber DK, Samardjiev IJ, Nasipak BT, Padilla-Benavides T, Wu Q, Imbalzano AN, Nickerson JA, Bunnage ME, Müller S, Knapp S, Owen DR. Gerstenberger BS, et al. J Med Chem. 2016 May 26;59(10):4800-11. doi: 10.1021/acs.jmedchem.6b00012. Epub 2016 May 3. J Med Chem. 2016. PMID: 27115555 Free PMC article.
2,6-Diisopropyl-anilinium chloride.
Samardjiev I, Samas B. Samardjiev I, et al. Acta Crystallogr Sect E Struct Rep Online. 2008 Jul 12;64(Pt 8):o1480. doi: 10.1107/S160053680801790X. Acta Crystallogr Sect E Struct Rep Online. 2008. PMID: 21203192 Free PMC article.
The design and synthesis of a potent glucagon receptor antagonist with favorable physicochemical and pharmacokinetic properties as a candidate for the treatment of type 2 diabetes mellitus.
Guzman-Perez A, Pfefferkorn JA, Lee EC, Stevens BD, Aspnes GE, Bian J, Didiuk MT, Filipski KJ, Moore D, Perreault C, Sammons MF, Tu M, Brown J, Atkinson K, Litchfield J, Tan B, Samas B, Zavadoski WJ, Salatto CT, Treadway J. Guzman-Perez A, et al. Bioorg Med Chem Lett. 2013 May 15;23(10):3051-8. doi: 10.1016/j.bmcl.2013.03.014. Epub 2013 Mar 13. Bioorg Med Chem Lett. 2013. PMID: 23562063
Discovery of a clinical candidate from the structurally unique dioxa-bicyclo[3.2.1]octane class of sodium-dependent glucose cotransporter 2 inhibitors.
Mascitti V, Maurer TS, Robinson RP, Bian J, Boustany-Kari CM, Brandt T, Collman BM, Kalgutkar AS, Klenotic MK, Leininger MT, Lowe A, Maguire RJ, Masterson VM, Miao Z, Mukaiyama E, Patel JD, Pettersen JC, Préville C, Samas B, She L, Sobol Z, Steppan CM, Stevens BD, Thuma BA, Tugnait M, Zeng D, Zhu T. Mascitti V, et al. Among authors: samas b. J Med Chem. 2011 Apr 28;54(8):2952-60. doi: 10.1021/jm200049r. Epub 2011 Mar 30. J Med Chem. 2011. PMID: 21449606
Rational design and synthesis of 4-((1R,2R)-2-hydroxycyclohexyl)-2(trifluoromethyl)benzonitrile (PF-998425), a novel, nonsteroidal androgen receptor antagonist devoid of phototoxicity for dermatological indications.
Li JJ, Iula DM, Nguyen MN, Hu LY, Dettling D, Johnson TR, Du DY, Shanmugasundaram V, Van Camp JA, Wang Z, Harter WG, Yue WS, Boys ML, Wade KJ, Drummond EM, Samas BM, Lefker BA, Hoge GS, Lovdahl MJ, Asbill J, Carroll M, Meade MA, Ciotti SM, Krieger-Burke T. Li JJ, et al. Among authors: samas bm. J Med Chem. 2008 Nov 13;51(21):7010-4. doi: 10.1021/jm8009316. Epub 2008 Oct 16. J Med Chem. 2008. PMID: 18921992
Dopamine D3/D2 Receptor Antagonist PF-4363467 Attenuates Opioid Drug-Seeking Behavior without Concomitant D2 Side Effects.
Wager TT, Chappie T, Horton D, Chandrasekaran RY, Samas B, Dunn-Sims ER, Hsu C, Nawreen N, Vanase-Frawley MA, O'Connor RE, Schmidt CJ, Dlugolenski K, Stratman NC, Majchrzak MJ, Kormos BL, Nguyen DP, Sawant-Basak A, Mead AN. Wager TT, et al. ACS Chem Neurosci. 2017 Jan 18;8(1):165-177. doi: 10.1021/acschemneuro.6b00297. Epub 2016 Oct 21. ACS Chem Neurosci. 2017. PMID: 27715007
Synthesis and biological evaluation of amino-pyridines as androgen receptor antagonists for stimulating hair growth and reducing sebum production.
Hu LY, Lei HJ, Du D, Johnson TR, Fedij V, Kostlan C, Yue WS, Lovdahl M, Li JJ, Carroll M, Dettling D, Asbill J, Fan C, Wade K, Pocalyko D, Lapham K, Yalamanchili R, Samas B, Vrieze D, Ciotti S, Krieger-Burke T, Sliskovic D, Welgus H. Hu LY, et al. Bioorg Med Chem Lett. 2007 Oct 15;17(20):5693-7. doi: 10.1016/j.bmcl.2007.07.059. Epub 2007 Aug 19. Bioorg Med Chem Lett. 2007. PMID: 17766112
25 results