| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1375949 | Bioorganic & Medicinal Chemistry Letters | 2009 | 4 Pages |
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 α-Fas-induced liver injury.
Graphical abstractP4 derivatives of the oxamyl dipeptide caspase inhibitors are reported. Compounds 29 and 36 exhibited moderate membrane permeability and potent in vivo efficacy in an α-Fas-induced liver injury model.Figure optionsDownload full-size imageDownload as PowerPoint slide
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Authors
Hirokazu Ueno, Makoto Kawai, Hirohisa Shimokawa, Masako Hirota, Masashi Ohmi, Rie Sudo, Atsuko Ohta, Yoshimasa Arano, Kazunari Hattori, Takashi Ohmi, Naoto Kato, Midori Kojima, Yoshinobu Ueno, Mitsuko Yamamoto, Yukiko Moriguchi, Hiroyuki Eda,