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
Colletti, SL
Li, CS
Fisher, MH
Wyvratt, MJ
Meinke, PT
[J]. 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
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
[J]. 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
Sinclair, PJ
Wong, F
Staruch, MJ
Wiederrecht, G
Parsons, WH
Dumont, F
Wyvratt, M
[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 1996, 6 (18) : 2193 - 2196
[6] Apicidins: Novel cyclic tetrapeptides as coccidiostats and antimalarial agents from Fusarium pallidoroseum
Singh, SB
Zink, DL
Polishook, JD
Dombrowski, AW
DarkinRattray, SJ
Schmatz, DM
Goetz, MA
[J]. TETRAHEDRON LETTERS, 1996, 37 (45) : 8077 - 8080

← 1 →