316830-80-5Relevant academic research and scientific papers
Synthesis, calpain inhibitory activity, and cytotoxicity of P 2-substituted proline and thiaproline peptidyl aldehydes and peptidyl α-ketoamides
Korukonda, Rajani,Guan, Na,Dalton, James T.,Liu, Jiuyu,Donkor, Isaac O.
, p. 5282 - 5290 (2007/10/03)
Calpain is a cytosolic cysteine endopeptidase that has been implicated in a number of disorders including cancer. We have synthesized and studied the μ-calpain inhibitory activity and cytotoxicity of peptidyl aldehydes and peptidyl α-ketoamides with N-sub
Significance of hydrogen bonding at the S1′ subsite of calpain I
Donkor, Isaac O.,Zheng, Xiaozhang,Han, Jie,Lacy, Calvin,Miller, Duane D.
, p. 1753 - 1755 (2007/10/03)
α-Ketohydroxamates were synthesized as bioisosteres of α-ketoamides. The α-ketohydroxamates were generally more potent than the corresponding α-ketoamides. The potency of the compounds suggests that hydrogen bonding and steric bulk of substituents on the nitrogen atom of the ketoamide moiety influence calpain inhibition.
Synthesis and calpain inhibitory activity of α-ketoamides with 2,3-methanoleucine stereoisomers at the P2 position
Donkor, Isaac O.,Zheng, Xiaozhang,Miller, Duane D.
, p. 2497 - 2500 (2007/10/03)
A series of novel ketoamides incorporating all four 2,3-methanoleucine stereoisomers at the P2 position was synthesized. The compounds displayed a wide variation in K(i) values for inhibition of calpain I depending on the configuration of the P
