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Acetylenic TACE inhibitors. Part 1. SAR of the acyclic sulfonamide hydroxamates.
Levin JI, Chen JM, Cheung K, Cole D, Crago C, Santos ED, Du X, Khafizova G, MacEwan G, Niu C, Salaski EJ, Zask A, Cummons T, Sung A, Xu J, Zhang Y, Xu W, Ayral-Kaloustian S, Jin G, Cowling R, Barone D, Mohler KM, Black RA, Skotnicki JS. Levin JI, et al. Among authors: zhang y. Bioorg Med Chem Lett. 2003 Aug 18;13(16):2799-803. doi: 10.1016/s0960-894x(03)00514-6. Bioorg Med Chem Lett. 2003. PMID: 12873518
Identification of potent and selective TACE inhibitors via the S1 pocket.
Condon JS, Joseph-McCarthy D, Levin JI, Lombart HG, Lovering FE, Sun L, Wang W, Xu W, Zhang Y. Condon JS, et al. Among authors: zhang y. Bioorg Med Chem Lett. 2007 Jan 1;17(1):34-9. doi: 10.1016/j.bmcl.2006.10.004. Epub 2006 Oct 5. Bioorg Med Chem Lett. 2007. PMID: 17064892
Identification and characterization of 4-[[4-(2-butynyloxy)phenyl]sulfonyl]-N-hydroxy-2,2-dimethyl-(3S)thiomorpholinecarboxamide (TMI-1), a novel dual tumor necrosis factor-alpha-converting enzyme/matrix metalloprotease inhibitor for the treatment of rheumatoid arthritis.
Zhang Y, Xu J, Levin J, Hegen M, Li G, Robertshaw H, Brennan F, Cummons T, Clarke D, Vansell N, Nickerson-Nutter C, Barone D, Mohler K, Black R, Skotnicki J, Gibbons J, Feldmann M, Frost P, Larsen G, Lin LL. Zhang Y, et al. J Pharmacol Exp Ther. 2004 Apr;309(1):348-55. doi: 10.1124/jpet.103.059675. Epub 2004 Jan 12. J Pharmacol Exp Ther. 2004. PMID: 14718605
Characterization of (2R, 3S)-2-([[4-(2-butynyloxy)phenyl]sulfonyl]amino)-N,3-dihydroxybutanamide, a potent and selective inhibitor of TNF-alpha converting enzyme.
Zhang Y, Hegen M, Xu J, Keith JC Jr, Jin G, Du X, Cummons T, Sheppard BJ, Sun L, Zhu Y, Rao VR, Wang Q, Xu W, Cowling R, Nickerson-Nutter CL, Gibbons J, Skotnicki J, Lin LL, Levin J. Zhang Y, et al. Int Immunopharmacol. 2004 Dec 20;4(14):1845-57. doi: 10.1016/j.intimp.2004.08.003. Int Immunopharmacol. 2004. PMID: 15531300
The basal SAR of a novel insulin receptor activator.
Wood HB Jr, Black R, Salituro G, Szalkowski D, Li Z, Zhang Y, Moller DE, Zhang B, Jones AB. Wood HB Jr, et al. Among authors: zhang b, zhang y. Bioorg Med Chem Lett. 2000 Jun 5;10(11):1189-92. doi: 10.1016/s0960-894x(00)00206-7. Bioorg Med Chem Lett. 2000. PMID: 10866378
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