Novel inhibitors of the enzyme estrone sulfatase (ES)

被引：32

作者：

Ahmed, S ^{[1
]}

James, K ^{[1
]}

Owen, CP ^{[1
]}

Patel, CK ^{[1
]}

Patel, M ^{[1
]}

机构：

[1] Kingston Univ, Sch Chem & Pharmaceut Sci, Kingston upon Thames KT1 2EE, Surrey, England

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2001年 / 11卷 / 06期

关键词：

D O I：

10.1016/S0960-894X(01)00086-5

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

We report the initial results of our study into a series of simple 4-sulfamated phenyl alkyl ketones as potential inhibitors of the enzyme estrone sulfatase. The results of the study show that these compounds are potent inhibitors, possessing greater inhibitory activity than COUMATE, but weaker activity than EMATE. Furthermore, the compounds are observed to be irreversible inhibitors. (C) 2001 Elsevier Science Ltd. All rights reserved.

引用

页码：841 / 844

页数：4

共 9 条

[1] First report of the investigation into the importance of pKa in the inhibition of estrone sulfatase by sulfamate containing compounds [J].

Ahmed, S ;

James, K ;

Patel, CK .

BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS, 2000, 272 (02) :583-585

[2] Estrone sulfatase: Probing structural requirements for substrate and inhibitor recognition [J].

Anderson, C ;

Freeman, J ;

Lucas, LH ;

Farley, M ;

Dalhoumi, H ;

Widlanski, TS .

BIOCHEMISTRY, 1997, 36 (09) :2586-2594

[3] Aromatase inhibitors and their application in breast cancer treatment [J].

Brodie, AMH ;

Njar, VCO .

STEROIDS, 2000, 65 (04) :171-179

[4]

Feutrie ML, 1999, B CANCER, V86, P821

[5] Estrone sulfonates as inhibitors of estrone sulfatase [J].

Howarth, NM ;

Purohit, A ;

Reed, MJ ;

Potter, BVL .

STEROIDS, 1997, 62 (04) :346-350

[6] Steroid sulphatase: expression, isolation and inhibition for active-site identification studies [J].

Purohit, A ;

Potter, BVL ;

Parker, MG ;

Reed, MJ .

CHEMICO-BIOLOGICAL INTERACTIONS, 1998, 109 (1-3) :183-193

[7] Inhibition of placental estrone sulfatase activity and MCF-7 breast cancer cell proliferation by estrone-3-amino derivatives [J].

Selcer, KW ;

Jagannathan, S ;

Rhodes, ME ;

Li, PK .

JOURNAL OF STEROID BIOCHEMISTRY AND MOLECULAR BIOLOGY, 1996, 59 (01) :83-91

[8] Heteroatom-substituted analogues of the active-site directed inhibitor estra-1,3,5(10)-trien-17-one-3-sulphamate inhibit estrone sulphatase by a different mechanism [J].

Woo, LWL ;

Lightowler, M ;

Purohit, A ;

Reed, MJ ;

Potter, BVL .

JOURNAL OF STEROID BIOCHEMISTRY AND MOLECULAR BIOLOGY, 1996, 57 (1-2) :79-88

[9] Steroidal and nonsteroidal sulfamates as potent inhibitors of steroid sulfatase [J].

Woo, LWL ;

Howarth, NM ;

Purohit, A ;

Hejaz, HAM ;

Reed, MJ ;

Potter, BVL .

JOURNAL OF MEDICINAL CHEMISTRY, 1998, 41 (07) :1068-1083

← 1 →