Broad spectrum antiprotozoal agents that inhibit histone deacetylase: Structure-activity relationships of apicidin. Part 2

被引：60

作者：

Colletti, SL ^{[1
]}

Myers, RW ^{[1
]}

Darkin-Rattray, SJ ^{[1
]}

Gurnett, AM ^{[1
]}

Dulski, PM ^{[1
]}

Galuska, S ^{[1
]}

Allocco, JJ ^{[1
]}

Ayer, MB ^{[1
]}

Li, CS ^{[1
]}

Lim, J ^{[1
]}

Crumley, TM ^{[1
]}

Cannova, C ^{[1
]}

Schmatz, DM ^{[1
]}

Wyvratt, MJ ^{[1
]}

Fisher, MH ^{[1
]}

Meinke, PT ^{[1
]}

机构：

[1] Merck & Co Inc, Merck Res Labs, Dept Med Chem, Rahway, NJ 07065 USA

来源：

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

关键词：

D O I：

10.1016/S0960-894X(00)00605-3

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Recently isolated at Merck, apicidin inhibits both mammalian and protozoan histone deacetylases (HDACs). The conversion of apicidin, a nonselective nanomolar inhibitor of HDACs, into a series of picomolar indole-modified and parasite-selective tryptophan-replacement analogues is described within this structure-activity study. (C) 2001 Elsevier Science Ltd. All rights reserved.

引用

页码：113 / 117

页数：5

共 6 条

[1] Tryptophan-replacement and indole-modifed apicidins: synthesis of potent and selective antiprotozoal agents [J].

Colletti, SL ;

Li, CS ;

Fisher, MH ;

Wyvratt, MJ ;

Meinke, PT .

TETRAHEDRON LETTERS, 2000, 41 (41) :7825-7829

[2]

Colletti SL, 2001, BIOORG MED CHEM LETT, V11, P107, DOI 10.1016/S0960-894X(00)00604-1

[3] Apicidin: A novel antiprotozoal agent that inhibits parasite histone deacetylase [J].

DarkinRattray, SJ ;

Gurnett, AM ;

Myers, RW ;

Dulski, PM ;

Crumley, TM ;

Allocco, JJ ;

Cannova, C ;

Meinke, PT ;

Colletti, SL ;

Bednarek, MA ;

Singh, SB ;

Goetz, MA ;

Dombrowski, AW ;

Polishook, JD ;

Schmatz, DM .

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 1996, 93 (23) :13143-13147

[4]

MEINKE PT, 2000, IN PRESS J MED CHEM

[5] Preparation and in vitro activities of naphthyl and indolyl ether derivatives of the FK-506 related immunosuppressive macrolide ascomycin [J].

Sinclair, PJ ;

Wong, F ;

Staruch, MJ ;

Wiederrecht, G ;

Parsons, WH ;

Dumont, F ;

Wyvratt, M .

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 1996, 6 (18) :2193-2196

[6] Apicidins: Novel cyclic tetrapeptides as coccidiostats and antimalarial agents from Fusarium pallidoroseum [J].

Singh, SB ;

Zink, DL ;

Polishook, JD ;

Dombrowski, AW ;

DarkinRattray, SJ ;

Schmatz, DM ;

Goetz, MA .

TETRAHEDRON LETTERS, 1996, 37 (45) :8077-8080

← 1 →