Synthesis and activity of tetrapeptidic HTLV-I protease inhibitors possessing different P₃-cap moieties

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• 作者：Meihui Zhang ; Jeffrey-Tri Nguyen ; Henri-Obadja Kumada ; Tooru Kimura ; Maosheng Cheng ; Yoshio Hayashi ; Yoshiaki Kiso
• 关键词：HTLV-I ; ATL ; HIV-1 ; Aspartic protease inhibitor
• 刊名：Bioorganic and Medicinal Chemistry
• 出版年：2008
• 期刊代码：9_09680896
• 类别：ch
• 出版时间：15 May 2008
• 卷：16
• 期：10
• 页码：5795-5802
• 文件大小：311 K

摘要

The causative agent behind adult T-cell leukemia and tropical spastic paraparesis/HTLV-I-associated myelopathy is the human T-cell leukemia virus type 1 (HTLV-I). Tetrapeptidic HTLV-I protease inhibitors were designed on a previously reported potent inhibitor KNI-10516, with modifications at the P₃-cap moieties. All the inhibitors showed high HIV-1 protease inhibitory activity (over 98%inhibition at 50 nM) and most exhibited highly potent inhibition against HTLV-I protease (IC₅₀ values were less than 100 nM).