Conformational restriction of flexible ligands guided by the transferred NOE experiment: Potent macrocyclic inhibitors of farnesyltransferase

被引：70

作者：

Dinsmore, CJ ^{[1
]}

Bogusky, MJ

Culberson, JC

Bergman, JM

Homnick, CF

Zartman, CB

Mosser, SD

Schaber, MD

Robinson, RG

Koblan, KS

Huber, HE

Graham, SL

Hartman, GD

Huff, JR

Williams, TM

机构：

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

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

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

来源：

JOURNAL OF THE AMERICAN CHEMICAL SOCIETY | 2001年 / 123卷 / 09期

关键词：

D O I：

10.1021/ja003673q

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

引用

页码：2107 / 2108

页数：2

共 21 条

[1] BEESE LS, UNPUB
[2] CHENG Y, 1973, BIOCHEM PHARMACOL, V22, P3099
[3] Arylmethanesulfonates are convenient latent phenols in the nucleophilic aromatic substitution reaction
Dinsmore, CJ
Zartman, CB
[J]. TETRAHEDRON LETTERS, 1999, 40 (21) : 3989 - 3990
[4] Farnesyl protein transferase inhibitors and other therapies targeting the ras signal transduction pathway
End, DW
[J]. INVESTIGATIONAL NEW DRUGS, 1999, 17 (03) : 241 - 258
[5] BIOACTIVE CONFORMATION OF LUTEINIZING-HORMONE-RELEASING HORMONE - EVIDENCE FROM A CONFORMATIONALLY CONSTRAINED ANALOG
FREIDINGER, RM
VEBER, DF
PERLOW, DS
BROOKS, JR
SAPERSTEIN, R
[J]. SCIENCE, 1980, 210 (4470) : 656 - 658
[6] Anticancer drug targets: growth factors and growth factor signaling
Gibbs, JB
[J]. JOURNAL OF CLINICAL INVESTIGATION, 2000, 105 (01) : 9 - 13
[7] Go N., 1970, MACROMOLECULES, V3, P178, DOI DOI 10.1021/MA60014A012
[8] BIOACTIVE CONFORMATION OF STROMELYSIN INHIBITORS DETERMINED BY TRANSFERRED NUCLEAR OVERHAUSER EFFECTS
GONNELLA, NC
BOHACEK, R
ZHANG, XL
KOLOSSVARY, I
PARIS, CG
MELTON, R
WINTER, C
HU, SI
GANU, V
[J]. PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 1995, 92 (02) : 462 - 466
[9] ISOPRENOID ADDITION TO RAS PROTEIN IS THE CRITICAL MODIFICATION FOR ITS MEMBRANE ASSOCIATION AND TRANSFORMING ACTIVITY
KATO, K
COX, AD
HISAKA, MM
GRAHAM, SM
BUSS, JE
DER, CJ
[J]. PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 1992, 89 (14) : 6403 - 6407
[10] Lowering the entropic barrier for binding conformationally flexible inhibitors to enzymes
Khan, AR
Parrish, JC
Fraser, ME
Smith, WW
Bartlett, PA
James, MNG
[J]. BIOCHEMISTRY, 1998, 37 (48) : 16839 - 16845

← 1 2 3 →