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Page 1
Preclinical evaluation of an inhibitor of cytosolic phospholipase A2α for the treatment of asthma.
Hewson CA, Patel S, Calzetta L, Campwala H, Havard S, Luscombe E, Clarke PA, Peachell PT, Matera MG, Cazzola M, Page C, Abraham WM, Williams CM, Clark JD, Liu WL, Clarke NP, Yeadon M. Hewson CA, et al. Among authors: williams cm. J Pharmacol Exp Ther. 2012 Mar;340(3):656-65. doi: 10.1124/jpet.111.186379. Epub 2011 Dec 7. J Pharmacol Exp Ther. 2012. PMID: 22160268
Indole cytosolic phospholipase A2 alpha inhibitors: discovery and in vitro and in vivo characterization of 4-{3-[5-chloro-2-(2-{[(3,4-dichlorobenzyl)sulfonyl]amino}ethyl)-1-(diphenylmethyl)-1H-indol-3-yl]propyl}benzoic acid, efipladib.
McKew JC, Lee KL, Shen MW, Thakker P, Foley MA, Behnke ML, Hu B, Sum FW, Tam S, Hu Y, Chen L, Kirincich SJ, Michalak R, Thomason J, Ipek M, Wu K, Wooder L, Ramarao MK, Murphy EA, Goodwin DG, Albert L, Xu X, Donahue F, Ku MS, Keith J, Nickerson-Nutter CL, Abraham WM, Williams C, Hegen M, Clark JD. McKew JC, et al. J Med Chem. 2008 Jun 26;51(12):3388-413. doi: 10.1021/jm701467e. Epub 2008 May 23. J Med Chem. 2008. PMID: 18498150
Benzenesulfonamide indole inhibitors of cytosolic phospholipase A2alpha: optimization of in vitro potency and rat pharmacokinetics for oral efficacy.
Lee KL, Behnke ML, Foley MA, Chen L, Wang W, Vargas R, Nunez J, Tam S, Mollova N, Xu X, Shen MW, Ramarao MK, Goodwin DG, Nickerson-Nutter CL, Abraham WM, Williams C, Clark JD, McKew JC. Lee KL, et al. Bioorg Med Chem. 2008 Feb 1;16(3):1345-58. doi: 10.1016/j.bmc.2007.10.060. Epub 2007 Oct 22. Bioorg Med Chem. 2008. PMID: 17998165
Matrix metalloproteinase-12 is a therapeutic target for asthma in children and young adults.
Mukhopadhyay S, Sypek J, Tavendale R, Gartner U, Winter J, Li W, Page K, Fleming M, Brady J, O'Toole M, Macgregor DF, Goldman S, Tam S, Abraham W, Williams C, Miller DK, Palmer CN. Mukhopadhyay S, et al. J Allergy Clin Immunol. 2010 Jul;126(1):70-6.e16. doi: 10.1016/j.jaci.2010.03.027. Epub 2010 May 23. J Allergy Clin Immunol. 2010. PMID: 20546881
Diazine indole acetic acids as potent, selective, and orally bioavailable antagonists of chemoattractant receptor homologous molecule expressed on Th2 cells (CRTH2) for the treatment of allergic inflammatory diseases.
Kaila N, Huang A, Moretto A, Follows B, Janz K, Lowe M, Thomason J, Mansour TS, Hubeau C, Page K, Morgan P, Fish S, Xu X, Williams C, Saiah E. Kaila N, et al. J Med Chem. 2012 Jun 14;55(11):5088-109. doi: 10.1021/jm300007n. Epub 2012 May 31. J Med Chem. 2012. PMID: 22651823
Discovery of isoquinolinone indole acetic acids as antagonists of chemoattractant receptor homologous molecule expressed on Th2 cells (CRTH2) for the treatment of allergic inflammatory diseases.
Kaila N, Follows B, Leung L, Thomason J, Huang A, Moretto A, Janz K, Lowe M, Mansour TS, Hubeau C, Page K, Morgan P, Fish S, Xu X, Williams C, Saiah E. Kaila N, et al. J Med Chem. 2014 Feb 27;57(4):1299-322. doi: 10.1021/jm401509e. Epub 2014 Feb 10. J Med Chem. 2014. PMID: 24512187
Discovery of potent and selective matrix metalloprotease 12 inhibitors for the potential treatment of chronic obstructive pulmonary disease (COPD).
Wu Y, Li J, Wu J, Morgan P, Xu X, Rancati F, Vallese S, Raveglia L, Hotchandani R, Fuller N, Bard J, Cunningham K, Fish S, Krykbaev R, Tam S, Goldman SJ, Williams C, Mansour TS, Saiah E, Sypek J, Li W. Wu Y, et al. Bioorg Med Chem Lett. 2012 Jan 1;22(1):138-43. doi: 10.1016/j.bmcl.2011.11.046. Epub 2011 Nov 20. Bioorg Med Chem Lett. 2012. PMID: 22153340
A selective matrix metalloprotease 12 inhibitor for potential treatment of chronic obstructive pulmonary disease (COPD): discovery of (S)-2-(8-(methoxycarbonylamino)dibenzo[b,d]furan-3-sulfonamido)-3-methylbutanoic acid (MMP408).
Li W, Li J, Wu Y, Wu J, Hotchandani R, Cunningham K, McFadyen I, Bard J, Morgan P, Schlerman F, Xu X, Tam S, Goldman SJ, Williams C, Sypek J, Mansour TS. Li W, et al. J Med Chem. 2009 Apr 9;52(7):1799-802. doi: 10.1021/jm900093d. J Med Chem. 2009. PMID: 19278250
1,178 results