AMINOPHOSPHONIC ACID-CONTAINING INHIBITORS OF HUMAN COLLAGENASE - MODIFICATION OF THE P-1 RESIDUE

被引：21

作者：

HUNTER, DJ

BIRD, J

CASSIDY, F

DEMELLO, RC

HARPER, GP

KARRAN, EH

MARKWELL, RE

MILESWILLIAMS, AJ

WARD, RW

机构：

[1] SmithKline Beecham Pharmaceuticals, Department of Medicinal Chemistry, Harlow, Essex CM19 5AW, New Frontiers Science Park, Third Ave.

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1994年 / 4卷 / 24期

关键词：

D O I：

10.1016/S0960-894X(01)80823-4

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of peptidomimetic aminophosphonic acid derivatives was synthesized and evaluated in vitro for inhibition of human fibroblast collagenase activity. Incorporation of a bromonaphthalimidoethyl moiety at the P-1 position led to potent inhibitors, such as 14a (IC50 0.02 mu M).

引用

页码：2833 / 2836

页数：4

共 12 条

[1] SYNTHESIS OF ORGANOPHOSPHORUS COMPOUNDS VIA SILYL ESTERS OF PHOSPHORUS-ACIDS
AFARINKIA, K
REES, CW
CADOGAN, JIG
[J]. TETRAHEDRON, 1990, 46 (20) : 7175 - 7196
[2] SYNTHESIS OF NOVEL N-PHOSPHONOALKYL DIPEPTIDE INHIBITORS OF HUMAN COLLAGENASE
BIRD, J
DEMELLO, RC
HARPER, GP
HUNTER, DJ
KARRAN, EH
MARKWELL, RE
MILESWILLIAMS, AJ
RAHMAN, SS
WARD, RW
[J]. JOURNAL OF MEDICINAL CHEMISTRY, 1994, 37 (01) : 158 - 169
[3] MATRIX METALLOPROTEINASES - A REVIEW
BIRKEDALHANSEN, H
MOORE, WGI
BODDEN, MK
WINDSOR, LJ
BIRKEDALHANSEN, B
DECARLO, A
ENGLER, JA
[J]. CRITICAL REVIEWS IN ORAL BIOLOGY & MEDICINE, 1993, 4 (02) : 197 - 250
[4] BROADHURST MJ, 1988, Patent No. 276436
[5] MATRIX METALLOPROTEINASE INHIBITORS CONTAINING A (CARBOXYALKYL)AMINO ZINC LIGAND - MODIFICATION OF THE P1 AND P2' RESIDUES
BROWN, FK
BROWN, PJ
BICKETT, DM
CHAMBERS, CL
DAVIES, HG
DEATON, DN
DREWRY, D
FOLEY, M
MCELROY, AB
GREGSON, M
MCGEEHAN, GM
MYERS, PL
NORTON, D
SALOVICH, JM
SCHOENEN, FJ
WARD, P
[J]. JOURNAL OF MEDICINAL CHEMISTRY, 1994, 37 (05) : 674 - 688
[6] BROWN PA, 1994, J CELL BIOCHEM, P120
[7] DOCHERTY AJP, 1990, ANN RHEUM DIS, P469
[8] Galardy R E, 1992, Matrix Suppl, V1, P259
[9] HENDERSON B, 1990, Drugs of the Future, V15, P495
[10] OKADA Y, 1986, J BIOL CHEM, V261, P14245

← 1 2 →