Nortropinyl-arylsulfonylureas as novel, reversible inhibitors of human steroid sulfatase

被引：21
作者：
Nussbaumer, P
Geyl, D
Horvath, A
Lehr, P
Wolff, B
Billich, A
机构：
[1] Novartis Res Inst Vienna, A-1235 Vienna, Austria
[2] Novartis Inst Biomed Res, Basel, Switzerland
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2003年 / 13卷 / 21期
关键词：
D O I：
10.1016/j.bmcl.2003.08.019
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Steroid sulfatase (STS) has emerged as an attractive target for a range of estrogen- and androgen- dependent diseases. Searching for novel chemotypes as STS inhibitors, we identified nortropinyl-arylsulfonylurea 3 as a hit from high-throughput screening. A series of analogues was prepared in order to explore the essential structural elements for STS inhibition, and first structure-activity relationships were established. Mechanistic investigations revealed that the compounds are reversible, competitive inhibitors of STS. (C) 2003 Elsevier Ltd. All rights reserved.
引用
收藏
页码：3673 / 3677
页数：5
相关论文
共 50 条
  • [41] STEROID SULFATASE ACTIVITY IN HUMAN-LEUKOCYTES
    MIYAKAWA, I
    KAWANO, Y
    TANIYAMA, K
    MORI, N
    GYNECOLOGIC AND OBSTETRIC INVESTIGATION, 1994, 38 (03) : 191 - 193
  • [42] STEROID SULFATASE ACTIVITIES IN HUMAN BREAST TUMORS
    DAO, TL
    HAYES, C
    LIBBY, PR
    PROCEEDINGS OF THE SOCIETY FOR EXPERIMENTAL BIOLOGY AND MEDICINE, 1974, 146 (02): : 381 - 384
  • [43] Nonsteroidal compounds designed to mimic potent steroid sulfatase inhibitors
    Ciobanu, LC
    Luu-The, V
    Poirier, D
    JOURNAL OF STEROID BIOCHEMISTRY AND MOLECULAR BIOLOGY, 2002, 80 (03) : 339 - 353
  • [44] Steroid sulfatase inhibitors: promising new therapy for breast cancer
    Sadozai, Hassan
    JOURNAL OF THE PAKISTAN MEDICAL ASSOCIATION, 2013, 63 (04) : 509 - 515
  • [45] Steroid Sulfatase Inhibitors Based on Phosphate and Thiophosphate Flavone Analogs
    Kozak, Witold
    Dasko, Mateusz
    Maslyk, Maciej
    Kubinski, Konrad
    Rachon, Janusz
    Demkowicz, Sebastian
    DRUG DEVELOPMENT RESEARCH, 2015, 76 (08) : 450 - 462
  • [46] Steroid sulfatase and estrogen sulfotransferase in human carcinomas
    Suzuki, Takashi
    Miki, Yasuhiro
    Nakamura, Yasuhiro
    Ito, Kiyoshi
    Sasano, Hironobu
    MOLECULAR AND CELLULAR ENDOCRINOLOGY, 2011, 340 (02) : 148 - 153
  • [47] HUMAN GLUCOSAMINE-6-SULFATASE CDNA REVEALS HOMOLOGY WITH STEROID SULFATASE
    ROBERTSON, DA
    FREEMAN, C
    NELSON, PV
    MORRIS, CP
    HOPWOOD, JJ
    BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS, 1988, 157 (01) : 218 - 224
  • [48] Novel D-ring modified steroid derivatives as potent, non-estrogenic, steroid sulfatase inhibitors with in vivo activity
    Fischer, DS
    Chander, SK
    Woo, LWL
    Fenton, JC
    Purohit, A
    Reed, MJ
    Potter, BVL
    JOURNAL OF STEROID BIOCHEMISTRY AND MOLECULAR BIOLOGY, 2003, 84 (2-3) : 343 - 349
  • [49] The use of steroid sulfatase inhibitors as a novel therapeutic strategy against hormone-dependent endometrial cancer
    Foster, Paul A.
    Woo, L. W. Lawrence
    Potter, Barry V. L.
    Reed, Michael J.
    Purohit, Atul
    ENDOCRINOLOGY, 2008, 149 (08) : 4035 - 4042
  • [50] In vitro and in vivo models for the evaluation of new inhibitors of human steroid sulfatase, devoid of residual estrogenic activity
    Shields-Botella, J
    Bonnet, P
    Duc, I
    Duranti, E
    Meschi, S
    Cardinali, S
    Prouheze, P
    Chaigneau, AM
    Duranti, V
    Gribaudo, S
    Rivière, A
    Mengual, L
    Carniato, D
    Cecchet, L
    Lafay, J
    Rondot, B
    Sandri, J
    Pascal, JC
    Delansorne, R
    JOURNAL OF STEROID BIOCHEMISTRY AND MOLECULAR BIOLOGY, 2003, 84 (2-3) : 327 - 335
12345