Solid-phase synthesis of cyclic alkoxyketones, inhibitors of the cysteine protease cathepsin K

被引：19

作者：

Fenwick, AE ^{[1
]}

Garnier, B ^{[1
]}

Gribble, AD ^{[1
]}

Ife, RJ ^{[1
]}

Rawlings, AD ^{[1
]}

Witherington, J ^{[1
]}

机构：

[1] SmithKline Beecham Pharmaceut, Dept Med Chem, Harlow CM19 5AD, Essex, England

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2001年 / 11卷 / 02期

关键词：

D O I：

10.1016/S0960-894X(00)00626-0

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Using solid-phase synthesis, a library of novel cyclic alkoxyketones has been constructed which show strong inhibitory activity against the cysteine protease, cathepsin K (EC 3.4.22.38). (C) 2001 Published by Elsevier Science Ltd.

引用

页码：195 / 198

页数：4

共 14 条

[1]

ALBERICIO F, 1987, INT J PEPT PROT RES, V30, P206

[2] Proteolytic activity of human osteoclast cathepsin K - Expression, purification, activation, and substrate identification [J].

Bossard, MJ ;

Tomaszek, TA ;

Thompson, SK ;

Amegadzie, BY ;

Hanning, CR ;

Jones, C ;

Kurdyla, JT ;

McNulty, DE ;

Drake, FH ;

Gowen, M ;

Levy, MA .

JOURNAL OF BIOLOGICAL CHEMISTRY, 1996, 271 (21) :12517-12524

[3] Cathepsin K, but not cathepsins B, L, or S, is abundantly expressed in human osteoclasts [J].

Drake, FH ;

Dodds, RA ;

James, IE ;

Connor, JR ;

Debouck, C ;

Richardson, S ;

LeeRykaczewski, E ;

Coleman, L ;

Rieman, D ;

Barthlow, R ;

Hastings, G ;

Gowen, M .

JOURNAL OF BIOLOGICAL CHEMISTRY, 1996, 271 (21) :12511-12516

[4] GENERAL-METHOD FOR RAPID SYNTHESIS OF MULTICOMPONENT PEPTIDE MIXTURES [J].

FURKA, A ;

SEBESTYEN, F ;

ASGEDOM, M ;

DIBO, G .

INTERNATIONAL JOURNAL OF PEPTIDE AND PROTEIN RESEARCH, 1991, 37 (06) :487-493

[5]

GRIBBLE AD, Patent No. 9850533

[6] A NEW TYPE OF SYNTHETIC PEPTIDE LIBRARY FOR IDENTIFYING LIGAND-BINDING ACTIVITY [J].

LAM, KS ;

SALMON, SE ;

HERSH, EM ;

HRUBY, VJ ;

KAZMIERSKI, WM ;

KNAPP, RJ .

NATURE, 1991, 354 (6348) :82-84

[7] Conformationally constrained 1,3-diamino ketones: A series of potent inhibitors of the cysteine protease cathepsin K [J].

Marquis, RW ;

Yamashita, DS ;

Ru, Y ;

LoCastro, SM ;

Oh, HJ ;

Erhard, KF ;

DesJarlais, RL ;

Head, MS ;

Smith, WW ;

Zhao, BG ;

Janson, CA ;

Abdel-Meguid, SS ;

Tomaszek, TA ;

Levy, MA ;

Veber, DF .

JOURNAL OF MEDICINAL CHEMISTRY, 1998, 41 (19) :3563-3567

[8]

MARQUIS RW, 1999, BIOORG MED CHEM LETT, V7, P599

[9]

MARQUIS RW, UNPUB J MED CHEM

[10]

MCKERROW JH, 1997, PERSPECT DRUG DISCOV, V6, P1

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