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Page 1
Conformationally constrained o-tolylpiperazine camphorsulfonamide oxytocin antagonists. Structural modifications that provide high receptor affinity and suggest a bioactive conformation.
Williams PD, Ball RG, Clineschmidt BV, Culberson JC, Erb JM, Freidinger RM, Pawluczyk JM, Perlow DS, Pettibone DJ, Veber DF. Williams PD, et al. Among authors: culberson jc. Bioorg Med Chem. 1994 Sep;2(9):971-85. doi: 10.1016/s0968-0896(00)82046-5. Bioorg Med Chem. 1994. PMID: 7712132
1-((7,7-Dimethyl-2(S)-(2(S)-amino-4-(methylsulfonyl)butyramido)bicyclo [2.2.1]-heptan-1(S)-yl)methyl)sulfonyl)-4-(2-methylphenyl)piperaz ine (L-368,899): an orally bioavailable, non-peptide oxytocin antagonist with potential utility for managing preterm labor.
Williams PD, Anderson PS, Ball RG, Bock MG, Carroll L, Chiu SH, Clineschmidt BV, Culberson JC, Erb JM, Evans BE, et al. Williams PD, et al. Among authors: culberson jc. J Med Chem. 1994 Mar 4;37(5):565-71. doi: 10.1021/jm00031a004. J Med Chem. 1994. PMID: 8126695
Evaluation of amino acid-based linkers in potent macrocyclic inhibitors of farnesyl-protein transferase.
Beshore DC, Bell IM, Dinsmore CJ, Homnick CF, Culberson JC, Robinson RG, Fernandes C, Walsh ES, Abrams MT, Bhimnathwala HG, Davide JP, Ellis-Hutchings MS, Huber HA, Koblan KS, Buser CA, Kohl NE, Lobell RB, Chen IW, McLoughlin DA, Olah TV, Graham SL, Hartman GD, Williams TM. Beshore DC, et al. Among authors: culberson jc. Bioorg Med Chem Lett. 2001 Jul 23;11(14):1817-21. doi: 10.1016/s0960-894x(01)00340-7. Bioorg Med Chem Lett. 2001. PMID: 11459639
Novel oxazolidinone calcitonin gene-related peptide (CGRP) receptor antagonists for the acute treatment of migraine.
Crowley BM, Stump CA, Nguyen DN, Potteiger CM, McWherter MA, Paone DV, Quigley AG, Bruno JG, Cui D, Culberson JC, Danziger A, Fandozzi C, Gauvreau D, Kemmerer AL, Menzel K, Moore EL, Mosser SD, Reddy V, White RB, Salvatore CA, Kane SA, Bell IM, Selnick HG, Fraley ME, Burgey CS. Crowley BM, et al. Among authors: culberson jc. Bioorg Med Chem Lett. 2015 Nov 1;25(21):4777-4781. doi: 10.1016/j.bmcl.2015.07.021. Epub 2015 Jul 14. Bioorg Med Chem Lett. 2015. PMID: 26231160
Non-thiol 3-aminomethylbenzamide inhibitors of farnesyl-protein transferase.
Ciccarone TM, MacTough SC, Williams TM, Dinsmore CJ, O'Neill TJ, Shah D, Culberson JC, Koblan KS, Kohl NE, Gibbs JB, Oliff AI, Graham SL, Hartman GD. Ciccarone TM, et al. Among authors: culberson jc. Bioorg Med Chem Lett. 1999 Jul 19;9(14):1991-6. doi: 10.1016/s0960-894x(99)00323-6. Bioorg Med Chem Lett. 1999. PMID: 10450968
Design and biological activity of (S)-4-(5-([1-(3-chlorobenzyl)-2-oxopyrrolidin-3-ylamino]methyl)imidazol-1-ylmethyl)benzonitrile, a 3-aminopyrrolidinone farnesyltransferase inhibitor with excellent cell potency.
Bell IM, Gallicchio SN, Abrams M, Beshore DC, Buser CA, Culberson JC, Davide J, Ellis-Hutchings M, Fernandes C, Gibbs JB, Graham SL, Hartman GD, Heimbrook DC, Homnick CF, Huff JR, Kassahun K, Koblan KS, Kohl NE, Lobell RB, Lynch JJ Jr, Miller PA, Omer CA, Rodrigues AD, Walsh ES, Williams TM. Bell IM, et al. Among authors: culberson jc. J Med Chem. 2001 Aug 30;44(18):2933-49. doi: 10.1021/jm010156p. J Med Chem. 2001. PMID: 11520202
Molecular model of the alpha(IIb)beta(3) integrin.
Feuston BP, Culberson JC, Hartman GD. Feuston BP, et al. Among authors: culberson jc. J Med Chem. 2003 Dec 4;46(25):5316-25. doi: 10.1021/jm030146j. J Med Chem. 2003. PMID: 14640540
Macrocyclic piperazinones as potent dual inhibitors of farnesyltransferase and geranylgeranyltransferase-I.
Dinsmore CJ, Zartman CB, Bergman JM, Abrams MT, Buser CA, Culberson JC, Davide JP, Ellis-Hutchings M, Fernandes C, Graham SL, Hartman GD, Huber HE, Lobell RB, Mosser SD, Robinson RG, Williams TM. Dinsmore CJ, et al. Among authors: culberson jc. Bioorg Med Chem Lett. 2004 Feb 9;14(3):639-43. doi: 10.1016/j.bmcl.2003.11.051. Bioorg Med Chem Lett. 2004. PMID: 14741259
45 results