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Page 1
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: black ra. 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
Synthesis and SAR of bicyclic heteroaryl hydroxamic acid MMP and TACE inhibitors.
Zask A, Gu Y, Albright JD, Du X, Hogan M, Levin JI, Chen JM, Killar LM, Sung A, DiJoseph JF, Sharr MA, Roth CE, Skala S, Jin G, Cowling R, Mohler KM, Barone D, Black R, March C, Skotnicki JS. Zask A, et al. Bioorg Med Chem Lett. 2003 Apr 17;13(8):1487-90. doi: 10.1016/s0960-894x(03)00127-6. Bioorg Med Chem Lett. 2003. PMID: 12668018
The discovery of anthranilic acid-based MMP inhibitors. Part 3: incorporation of basic amines.
Levin JI, Chen JM, Du MT, Nelson FC, Wehr T, DiJoseph JF, Killar LM, Skala S, Sung A, Sharr MA, Roth CE, Jin G, Cowling R, Di L, Sherman M, Xu ZB, March CJ, Mohler KM, Black RA, Skotnicki JS. Levin JI, et al. Among authors: black ra. Bioorg Med Chem Lett. 2001 Nov 19;11(22):2975-8. doi: 10.1016/s0960-894x(01)00601-1. Bioorg Med Chem Lett. 2001. PMID: 11677139
The discovery of anthranilic acid-based MMP inhibitors. Part 2: SAR of the 5-position and P1(1) groups.
Levin JI, Chen J, Du M, Hogan M, Kincaid S, Nelson FC, Venkatesan AM, Wehr T, Zask A, DiJoseph J, Killar LM, Skala S, Sung A, Sharr M, Roth C, Jin G, Cowling R, Mohler KM, Black RA, March CJ, Skotnicki JS. Levin JI, et al. Among authors: black ra. Bioorg Med Chem Lett. 2001 Aug 20;11(16):2189-92. doi: 10.1016/s0960-894x(01)00419-x. Bioorg Med Chem Lett. 2001. PMID: 11514167
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
Substrate specificity and inducibility of TACE (tumour necrosis factor alpha-converting enzyme) revisited: the Ala-Val preference, and induced intrinsic activity.
Black RA, Doedens JR, Mahimkar R, Johnson R, Guo L, Wallace A, Virca D, Eisenman J, Slack J, Castner B, Sunnarborg SW, Lee DC, Cowling R, Jin G, Charrier K, Peschon JJ, Paxton R. Black RA, et al. Biochem Soc Symp. 2003;(70):39-52. doi: 10.1042/bss0700039. Biochem Soc Symp. 2003. PMID: 14587281 Review.
260 results