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Synthesis and structure-activity relationships of oxamyl dipeptide caspase inhibitors developed for the treatment of liver disease.
Ueno, Hirokazu; Kawai, Makoto; Shimokawa, Hirohisa; Hirota, Masako; Ohmi, Masashi; Sudo, Rie; Ohta, Atsuko; Arano, Yoshimasa; Hattori, Kazunari; Ohmi, Takashi; Kato, Naoto; Kojima, Midori; Ueno, Yoshinobu; Yamamoto, Mitsuko; Moriguchi, Yukiko; Eda, Hiroyuki; Masubuchi, Kazunao.
Bioorg Med Chem Lett ; 19(1): 199-202, 2009 Jan 01.
Article in English | MEDLINE | ID: mdl-19013793

ABSTRACT

The P4 region of a series of oxamyl dipeptide caspase inhibitors was optimized by the combination of anti-apoptotic activity in the Jurkat/Fas (JFas) cellular assay and membrane permeability in the PAMPA assay. Two highly potent anti-apoptotic agents with moderate membrane permeability, 29 and 36, showed strong in vivo efficacy in a murine model of alpha-Fas-induced liver injury.


Subject(s)
Caspase Inhibitors , Cysteine Proteinase Inhibitors/chemical synthesis , Liver Diseases/drug therapy , Animals , Apoptosis/drug effects , Cell Membrane Permeability/drug effects , Cysteine Proteinase Inhibitors/pharmacology , Humans , Jurkat Cells , Mice , Structure-Activity Relationship , fas Receptor
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