Non-thiol 3-aminomethylbenzamide inhibitors of farnesyl-protein transferase

被引：34

作者：

Ciccarone, TM

MacTough, SC

Williams, TM

Dinsmore, CJ

O'Neill, TJ

Shah, D

Culberson, JC

Koblan, KS

Kohl, NE

Gibbs, JB

Oliff, AI

Graham, SL

Hartman, GD

机构：

[1] Merck Res Labs, Dept Med Chem, W Point, PA 19486 USA

[2] Merck Res Labs, Dept Canc Res, W Point, PA 19486 USA

[3] Merck Res Labs, Dept Mol Syst, W Point, PA 19486 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1999年 / 9卷 / 14期

关键词：

D O I：

10.1016/S0960-894X(99)00323-6

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The design and syntheses of non-thiol inhibitors of farnesyl-protein transferase are described. Substitutions on an imidazolylmethyl-AMBA-methionine template gave a highly potent and cell active inhibitor. (C) 1999 Elsevier Science Ltd. All rights reserved.

引用

页码：1991 / 1996

页数：6

共 31 条

[1] ANTHONY NJ, IN PRESS J MED CHEM
[2] Potent and selective non-cysteine-containing inhibitors of protein farnesyltransferase
Augeri, DJ
O'Connor, SJ
Janowick, D
Szczepankiewicz, B
Sullivan, G
Larsen, J
Kalvin, D
Cohen, J
Devine, E
Zhang, HC
Cherian, S
Saeed, B
Ng, SC
Rosenberg, S
[J]. JOURNAL OF MEDICINAL CHEMISTRY, 1998, 41 (22) : 4288 - 4300
[3] RAS GENES
BARBACID, M
[J]. ANNUAL REVIEW OF BIOCHEMISTRY, 1987, 56 : 779 - 827
[4] Potent, non-thiol inhibitors of farnesyltransferase
Breslin, MJ
deSolms, SJ
Giuliani, EA
Stokker, GE
Graham, SL
Pompliano, DL
Mosser, SD
Hamilton, KA
Hutchinson, JH
[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 1998, 8 (23) : 3311 - 3316
[5] P21RAS IS MODIFIED BY A FARNESYL ISOPRENOID
CASEY, PJ
SOLSKI, PA
DER, CJ
BUSS, JE
[J]. PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 1989, 86 (21) : 8323 - 8327
[6] GIBBS JB, 1993, J BIOL CHEM, V268, P7617
[7] FARNESYLTRANSFERASE INHIBITORS - RAS RESEARCH YIELDS A POTENTIAL CANCER THERAPEUTIC
GIBBS, JB
OLIFF, A
KOHL, NE
[J]. CELL, 1994, 77 (02) : 175 - 178
[8] Graham S. L., 1995, EXPERT OPIN THER PAT, V5, P1269
[9] Inhibitors of protein farnesylation
Graham, SL
Williams, TM
[J]. EXPERT OPINION ON THERAPEUTIC PATENTS, 1996, 6 (12) : 1295 - 1304
[10] Potent, cell active, non-thiol tetrapeptide inhibitors of farnesyltransferase
Hunt, JT
Lee, VG
Leftheris, K
Seizinger, B
Carboni, J
Mabus, J
Ricca, C
Yan, N
Manne, V
[J]. JOURNAL OF MEDICINAL CHEMISTRY, 1996, 39 (02) : 353 - 358

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