Title of article
Dipeptidyl aspartyl fluoromethylketones as potent caspase-3 inhibitors: SAR of the P2 amino acid
Author/Authors
Yan Wang، نويسنده , , Jin-Chen Huang، نويسنده , , Zhang-Lin Zhou، نويسنده , , Wu Yang، نويسنده , , John Guastella، نويسنده , , John Drewe، نويسنده , , Sui-Xiong Cai، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2004
Pages
4
From page
1269
To page
1272
Abstract
This article describes the synthesis and biological evaluation of a series of dipeptidyl aspartyl fluoromethylketones as caspase-3 inhibitors. Structure–activity relationship (SAR) studies showed that for caspase-3 inhibition, Val is the best P2 amino acid. The SAR studies also showed that the Asp free carboxylic acid in P1 is important for caspase inhibiting activities, as well as for selectivity over other proteases.
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2004
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
794174
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