Identification of peptidomimetic HTLV-I protease inhibitors containing hydroxymethylcarbonyl (HMC) isostere as the transition-state mimic

被引：20

作者：

Maegawa, H ^{[1
]}

Kimura, T ^{[1
]}

Arii, Y ^{[1
]}

Matsui, Y ^{[1
]}

Kasai, S ^{[1
]}

Hayashi, Y ^{[1
]}

Kiso, Y ^{[1
]}

机构：

[1] Kyoto Pharmaceut Univ, Dept Med Chem, Ctr Frontier Res Med Sci, Yamashina Ku, Kyoto 6078412, Japan

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2004年 / 14卷 / 23期

关键词：

human T-cell leukemia virus type I (HTLV-I); adult T-cell leukemia (ATL); aspartic protease; inhibitor; hydroxymethylcarbonyl (HMC) isostere; chemical ligation;

D O I：

10.1016/j.bmcl.2004.09.034

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Towards the development of chemotherapy for the infection by human T-cell leukemia virus type I (HTLV-I), we have established evaluation systems for HTLV-I protease (PR) inhibitors using both recombinant and chemically synthesized HTLV-I PRs. Newly synthesized substrate-based inhibitors containing hydroxymethylcarbonyl (HMC) isostere showed potent anti-HTLV-I PR activity. (C) 2004 Elsevier Ltd. All rights reserved.

引用

页码：5925 / 5929

页数：5

共 27 条

[1] Solid-phase synthesis of HTLV-1 protease inhibitors containing hydroxyethylamine dipeptide isostere [J].