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Page 1
Acyl dipeptides as reversible caspase inhibitors. Part 2: further optimization.
Linton SD, Karanewsky DS, Ternansky RJ, Chen N, Guo X, Jahangiri KG, Kalish VJ, Meduna SP, Robinson ED, Ullman BR, Wu JC, Pham B, Kodandapani L, Smidt R, Diaz JL, Fritz LC, von Krosigk U, Roggo S, Schmitz A, Tomaselli KJ. Linton SD, et al. Bioorg Med Chem Lett. 2002 Oct 21;12(20):2973-5. doi: 10.1016/s0960-894x(02)00630-3. Bioorg Med Chem Lett. 2002. PMID: 12270186
Oxamyl dipeptide caspase inhibitors developed for the treatment of stroke.
Linton SD, Aja T, Allegrini PR, Deckwerth TL, Diaz JL, Hengerer B, Herrmann J, Jahangiri KG, Kallen J, Karanewsky DS, Meduna SP, Nalley K, Robinson ED, Roggo S, Rovelli G, Sauter A, Sayers RO, Schmitz A, Smidt R, Ternansky RJ, Tomaselli KJ, Ullman BR, Wiessner C, Wu JC. Linton SD, et al. Bioorg Med Chem Lett. 2004 May 17;14(10):2685-91. doi: 10.1016/j.bmcl.2003.12.106. Bioorg Med Chem Lett. 2004. PMID: 15109679
Structure-activity relationships within a series of caspase inhibitors. Part 2: Heterocyclic warheads.
Ullman BR, Aja T, Chen N, Diaz JL, Gu X, Herrmann J, Kalish VJ, Karanewsky DS, Kodandapani L, Krebs JJ, Linton SD, Meduna SP, Nalley K, Robinson ED, Roggo SP, Sayers RO, Schmitz A, Ternansky RJ, Tomaselli KJ, Wu JC. Ullman BR, et al. Among authors: linton sd. Bioorg Med Chem Lett. 2005 Aug 1;15(15):3632-6. doi: 10.1016/j.bmcl.2005.05.036. Bioorg Med Chem Lett. 2005. PMID: 15964758
First-in-class pan caspase inhibitor developed for the treatment of liver disease.
Linton SD, Aja T, Armstrong RA, Bai X, Chen LS, Chen N, Ching B, Contreras P, Diaz JL, Fisher CD, Fritz LC, Gladstone P, Groessl T, Gu X, Herrmann J, Hirakawa BP, Hoglen NC, Jahangiri KG, Kalish VJ, Karanewsky DS, Kodandapani L, Krebs J, McQuiston J, Meduna SP, Nalley K, Robinson ED, Sayers RO, Sebring K, Spada AP, Ternansky RJ, Tomaselli KJ, Ullman BR, Valentino KL, Weeks S, Winn D, Wu JC, Yeo P, Zhang CZ. Linton SD, et al. J Med Chem. 2005 Nov 3;48(22):6779-82. doi: 10.1021/jm050307e. J Med Chem. 2005. PMID: 16250635