schliessen

Filtern

 

Bibliotheken

Synthesis and Biological Evaluation of Spiro-δ-lactones as Inhibitors of 17β-Hydroxysteroid Dehydrogenase Type 2 (17β-HSD2)

17β-Hydroxysteroid dehydrogenase type 2 (17β-HSD2) catalyzes the oxidation of the potent estradiol (E2) to the less active estrogen estrone (E1). Inhibitors of this enzyme should maintain the local level of E2 in bone tissue when the E2 concentration in the circulation drops and therefore might be u... Full description

Journal Title: Letters in Drug Design & Discovery 2011, Vol.8(5), p.406-421
Main Author: Xu, Kuiying
Other Authors: Wetzel, Marie , W. Hartmann, Rolf , Marchais-Oberwinkler, Sandrine
Format: Electronic Article Electronic Article
Language: English
Subjects:
ID: ISSN: 1570-1808 ; E-ISSN: 1875-628X ; DOI: 10.2174/157018011795514230
Link: http://www.eurekaselect.com/openurl/content.php?genre=article&issn=15701808&volume=8&issue=5&spage=406
Zum Text:
SendSend as email Add to Book BagAdd to Book Bag
Staff View
recordid: bentham10.2174/157018011795514230
title: Synthesis and Biological Evaluation of Spiro-δ-lactones as Inhibitors of 17β-Hydroxysteroid Dehydrogenase Type 2 (17β-HSD2)
format: Article
creator:
  • Xu, Kuiying
  • Wetzel, Marie
  • W. Hartmann, Rolf
  • Marchais-Oberwinkler, Sandrine
subjects:
  • 17β-Hydroxysteroid Dehydrogenase Type 2 Inhibitors
  • Drug Design
  • Osteoporosis
  • Spiro-δ-Lactones
  • Steroidomimetics
  • Biological Evaluation
  • Spiro-Lactones
  • Inhibitors
  • 17-Hydroxysteroid
  • Dehydrogenase
  • Sdrs
  • Dihydrotestosterone
  • 4-Androstene-3,17-Dione
  • Spirolactone Derivatives
  • Aromatase Inhibitors
ispartof: Letters in Drug Design & Discovery, 2011, Vol.8(5), p.406-421
description: 17β-Hydroxysteroid dehydrogenase type 2 (17β-HSD2) catalyzes the oxidation of the potent estradiol (E2) to the less active estrogen estrone (E1). Inhibitors of this enzyme should maintain the local level of E2 in bone tissue when the E2 concentration in the circulation drops and therefore might be useful for the treatment of osteoporosis. In this work, novel non-steroidal spiro-δ-lactone compounds designed as 17β-HSD2 inhibitors were synthesized and their physicochemical and biological properties were investigated. These new spiro-δ-lactones are not sufficiently stable for further development and show low inhibition of the enzyme.
language: eng
source:
identifier: ISSN: 1570-1808 ; E-ISSN: 1875-628X ; DOI: 10.2174/157018011795514230
fulltext: fulltext
issn:
  • 1570-1808
  • 15701808
  • 1875-628X
  • 1875628X
url: Link


@attributes
ID1281845548
RANK0.07
NO1
SEARCH_ENGINEprimo_central_multiple_fe
SEARCH_ENGINE_TYPEPrimo Central Search Engine
LOCALfalse
PrimoNMBib
record
control
sourcerecordid10.2174/157018011795514230
sourceidbentham
recordidTN_bentham10.2174/157018011795514230
sourceformatXML
sourcesystemPC
pqid902376704
ingidben/lddd/2011/00000008/00000005/art00003
display
typearticle
titleSynthesis and Biological Evaluation of Spiro-δ-lactones as Inhibitors of 17β-Hydroxysteroid Dehydrogenase Type 2 (17β-HSD2)
creatorXu, Kuiying ; Wetzel, Marie ; W. Hartmann, Rolf ; Marchais-Oberwinkler, Sandrine
ispartofLetters in Drug Design & Discovery, 2011, Vol.8(5), p.406-421
identifier
subject17β-Hydroxysteroid Dehydrogenase Type 2 Inhibitors ; Drug Design ; Osteoporosis ; Spiro-δ-Lactones ; Steroidomimetics ; Biological Evaluation ; Spiro-Lactones ; Inhibitors ; 17-Hydroxysteroid ; Dehydrogenase ; Sdrs ; Dihydrotestosterone ; 4-Androstene-3,17-Dione ; Spirolactone Derivatives ; Aromatase Inhibitors
description17β-Hydroxysteroid dehydrogenase type 2 (17β-HSD2) catalyzes the oxidation of the potent estradiol (E2) to the less active estrogen estrone (E1). Inhibitors of this enzyme should maintain the local level of E2 in bone tissue when the E2 concentration in the circulation drops and therefore might be useful for the treatment of osteoporosis. In this work, novel non-steroidal spiro-δ-lactone compounds designed as 17β-HSD2 inhibitors were synthesized and their physicochemical and biological properties were investigated. These new spiro-δ-lactones are not sufficiently stable for further development and show low inhibition of the enzyme.
languageeng
source
version4
lds50peer_reviewed
links
openurl$$Topenurl_article
backlink$$Uhttp://www.eurekaselect.com/openurl/content.php?genre=article&issn=15701808&volume=8&issue=5&spage=406$$EView_record_at_Bentham_Science
openurlfulltext$$Topenurlfull_article
search
creatorcontrib
0Xu, Kuiying
1Wetzel, Marie
2W. Hartmann, Rolf
3Marchais-Oberwinkler, Sandrine
titleSynthesis and Biological Evaluation of Spiro-δ-lactones as Inhibitors of 17β-Hydroxysteroid Dehydrogenase Type 2 (17β-HSD2)
description17β-Hydroxysteroid dehydrogenase type 2 (17β-HSD2) catalyzes the oxidation of the potent estradiol (E2) to the less active estrogen estrone (E1). Inhibitors of this enzyme should maintain the local level of E2 in bone tissue when the E2 concentration in the circulation drops and therefore might be useful for the treatment of osteoporosis. In this work, novel non-steroidal spiro-δ-lactone compounds designed as 17β-HSD2 inhibitors were synthesized and their physicochemical and biological properties were investigated. These new spiro-δ-lactones are not sufficiently stable for further development and show low inhibition of the enzyme.
subject
017β-hydroxysteroid dehydrogenase type 2 inhibitors
1Drug design
2Osteoporosis
3Spiro-δ-lactones
4Steroidomimetics
5Biological Evaluation
6Spiro-lactones
7Inhibitors
817-Hydroxysteroid
9Dehydrogenase
10SDRs
11dihydrotestosterone
124-androstene-3,17-dione
13spirolactone derivatives
14aromatase inhibitors
general
010.2174/157018011795514230
1Bentham Science Publishers Ltd.
2English
3Bentham Science - Journals
sourceidbentham
recordidbentham10.2174/157018011795514230
issn
01570-1808
115701808
21875-628X
31875628X
rsrctypearticle
creationdate2011
addtitleLetters in Drug Design & Discovery
searchscopebentham
scopebentham
lsr30VSR-Enriched:[ingid, pqid]
sort
titleSynthesis and Biological Evaluation of Spiro-δ-lactones as Inhibitors of 17β-Hydroxysteroid Dehydrogenase Type 2 (17β-HSD2)
authorXu, Kuiying ; Wetzel, Marie ; W. Hartmann, Rolf ; Marchais-Oberwinkler, Sandrine
creationdate20110600
facets
frbrgroupid8273595022881916517
frbrtype5
languageeng
creationdate2011
topic
017β-hydroxysteroid dehydrogenase type 2 inhibitors
1Drug design
2Osteoporosis
3Spiro-δ-lactones
4Steroidomimetics
5Biological Evaluation
6Spiro-lactones
7Inhibitors
817-Hydroxysteroid
9Dehydrogenase
10SDRs
11dihydrotestosterone
124-androstene-3,17-dione
13spirolactone derivatives
14aromatase inhibitors
collectionBentham Science - Journals
prefilterarticles
rsrctypearticles
creatorcontrib
0Xu, Kuiying
1Wetzel, Marie
2W. Hartmann, Rolf
3Marchais-Oberwinkler, Sandrine
jtitleLetters in Drug Design & Discovery
toplevelpeer_reviewed
delivery
delcategoryRemote Search Resource
fulltextfulltext
addata
aulast
0Xu
1Wetzel
2W. Hartmann
3Marchais-Oberwinkler
aufirst
0Kuiying
1Marie
2Rolf
3Sandrine
au
0Xu, Kuiying
1Wetzel, Marie
2W. Hartmann, Rolf
3Marchais-Oberwinkler, Sandrine
atitleSynthesis and Biological Evaluation of Spiro-δ-lactones as Inhibitors of 17β-Hydroxysteroid Dehydrogenase Type 2 (17β-HSD2)
jtitleLetters in Drug Design & Discovery
risdate201106
volume8
issue5
spage406
epage421
pages406-421
issn1570-1808
eissn1875-628X
formatjournal
genrearticle
ristypeJOUR
abstract17β-Hydroxysteroid dehydrogenase type 2 (17β-HSD2) catalyzes the oxidation of the potent estradiol (E2) to the less active estrogen estrone (E1). Inhibitors of this enzyme should maintain the local level of E2 in bone tissue when the E2 concentration in the circulation drops and therefore might be useful for the treatment of osteoporosis. In this work, novel non-steroidal spiro-δ-lactone compounds designed as 17β-HSD2 inhibitors were synthesized and their physicochemical and biological properties were investigated. These new spiro-δ-lactones are not sufficiently stable for further development and show low inhibition of the enzyme.
pubBentham Science Publishers Ltd.
doi10.2174/157018011795514230
date2011-06