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Page 1
Potent N-(1,3-thiazol-2-yl)pyridin-2-amine vascular endothelial growth factor receptor tyrosine kinase inhibitors with excellent pharmacokinetics and low affinity for the hERG ion channel.
Bilodeau MT, Balitza AE, Koester TJ, Manley PJ, Rodman LD, Buser-Doepner C, Coll KE, Fernandes C, Gibbs JB, Heimbrook DC, Huckle WR, Kohl N, Lynch JJ, Mao X, McFall RC, McLoughlin D, Miller-Stein CM, Rickert KW, Sepp-Lorenzino L, Shipman JM, Subramanian R, Thomas KA, Wong BK, Yu S, Hartman GD. Bilodeau MT, et al. Among authors: mcloughlin d. J Med Chem. 2004 Dec 2;47(25):6363-72. doi: 10.1021/jm049697f. J Med Chem. 2004. PMID: 15566305
Potent 2-[(pyrimidin-4-yl)amine}-1,3-thiazole-5-carbonitrile-based inhibitors of VEGFR-2 (KDR) kinase.
Sisko JT, Tucker TJ, Bilodeau MT, Buser CA, Ciecko PA, Coll KE, Fernandes C, Gibbs JB, Koester TJ, Kohl N, Lynch JJ, Mao X, McLoughlin D, Miller-Stein CM, Rodman LD, Rickert KW, Sepp-Lorenzino L, Shipman JM, Thomas KA, Wong BK, Hartman GD. Sisko JT, et al. Among authors: mcloughlin d. Bioorg Med Chem Lett. 2006 Mar 1;16(5):1146-50. doi: 10.1016/j.bmcl.2005.11.089. Epub 2005 Dec 20. Bioorg Med Chem Lett. 2006. PMID: 16368234
Oxo-piperazine derivatives of N-arylpiperazinones as inhibitors of farnesyltransferase.
Dinsmore CJ, Bergman JM, Wei DD, Zartman CB, Davide JP, Greenberg IB, Liu D, O'Neill TJ, Gibbs JB, Koblan KS, Kohl NE, Lobell RB, Chen IW, McLoughlin DA, Olah TV, Graham SL, Hartman GD, Williams TM. Dinsmore CJ, et al. Among authors: mcloughlin da. Bioorg Med Chem Lett. 2001 Feb 26;11(4):537-40. doi: 10.1016/s0960-894x(00)00710-1. Bioorg Med Chem Lett. 2001. PMID: 11229765
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: mcloughlin da. 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
A combinatorial library of indinavir analogues and its in vitro and in vivo studies.
Cheng Y, Rano TA, Huening TT, Zhang F, Lu Z, Schleif WA, Gabryelski L, Olsen DB, Stahlhut M, Kuo LC, Lin JH, Xu X, Jin L, Olah TV, McLoughlin DA, King RC, Chapman KT, Tata JR. Cheng Y, et al. Bioorg Med Chem Lett. 2002 Feb 25;12(4):529-32. doi: 10.1016/s0960-894x(01)00824-1. Bioorg Med Chem Lett. 2002. PMID: 11844665
Characterization of non-nitrocatechol pan and isoform specific catechol-O-methyltransferase inhibitors and substrates.
Robinson RG, Smith SM, Wolkenberg SE, Kandebo M, Yao L, Gibson CR, Harrison ST, Polsky-Fisher S, Barrow JC, Manley PJ, Mulhearn JJ, Nanda KK, Schubert JW, Trotter BW, Zhao Z, Sanders JM, Smith RF, McLoughlin D, Sharma S, Hall DL, Walker TL, Kershner JL, Bhandari N, Hutson PH, Sachs NA. Robinson RG, et al. Among authors: mcloughlin d. ACS Chem Neurosci. 2012 Feb 15;3(2):129-40. doi: 10.1021/cn200109w. Epub 2011 Nov 14. ACS Chem Neurosci. 2012. PMID: 22860182 Free PMC article.
3-Pyridyloxypropanolamine agonists of the beta 3 adrenergic receptor with improved pharmacokinetic properties.
Weber AE, Ok HO, Alvaro RF, Candelore MR, Cascieri MA, Chiu SH, Deng L, Forrest MJ, Hom GJ, Hutchins JE, Kao J, MacIntyre DE, Mathvink RJ, McLoughlin D, Miller RR, Newbold RC, Olah TV, Parmee ER, Perkins L, Stearns RA, Strader CD, Szumiloski J, Tang YS, Tota L, Fisher MH, et al. Weber AE, et al. Among authors: mcloughlin d. Bioorg Med Chem Lett. 1998 Aug 18;8(16):2111-6. doi: 10.1016/s0960-894x(98)00381-3. Bioorg Med Chem Lett. 1998. PMID: 9873496
Synthesis and optimization of N-heterocyclic pyridinones as catechol-O-methyltransferase (COMT) inhibitors.
Zhao Z, Harrison ST, Schubert JW, Sanders JM, Polsky-Fisher S, Zhang NR, McLoughlin D, Gibson CR, Robinson RG, Sachs NA, Kandebo M, Yao L, Smith SM, Hutson PH, Wolkenberg SE, Barrow JC. Zhao Z, et al. Among authors: mcloughlin d. Bioorg Med Chem Lett. 2016 Jun 15;26(12):2952-2956. doi: 10.1016/j.bmcl.2016.03.095. Epub 2016 Apr 7. Bioorg Med Chem Lett. 2016. PMID: 27133481
299 results