Linked Life Data

6547488

Source:http://linkedlifedata.com/resource/pubmed/id/6547488

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
6
pubmed:dateCreated
1984-8-13
pubmed:abstractText
Derivatives of 19- azaandrostenedione (10 beta-amino-4- estrene -3,17-dione, 2) and 19-amino-4-androstene-3,17-dione (3) were synthesized as potential inhibitors of aromtase (estrogen synthetase). Compound 2 and its derivatives were synthesized from 3,17-dioxo-4-androsten-19-oic acid (5) via a Curtius rearrangement. Derivatives of 3 were synthesized from the intermediate 3,17-bis(ethylenedioxy)-5-androsten-19-al oxime (14), which was reduced to the corresponding amine (16) with Raney nickel. However, attempts to synthesize the parent compound, 3, from 16 by several different methods were unsuccessful. The compounds obtained were tested for inhibitory activity in the tritiated water assay for aromatase, with human placental microsomes as the enzyme source and [1-3H]-androst-4-ene-3,17-dione (83% 3H 1 beta) as the substrate. All of the compounds caused less than 20% inhibition of enzyme activity when tested at one and five times the substrate concentration (0.25 microM, 1.25 microM) and were poorer inhibitors than two known inhibitors, 7 alpha-[(p-aminophenyl)thio] androstenedione (7- APTA ) and 4-hydroxy-4-androstene-3,17-dione (4-OHA).
pubmed:grant
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Jun
pubmed:issn
0022-2623
pubmed:author
pubmed:issnType
Print
pubmed:volume
27
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
734-40
pubmed:dateRevised
2007-11-14
pubmed:meshHeading
pubmed:year
1984
pubmed:articleTitle
Synthesis and evaluation of 19-aza- and 19-aminoandrostenedione analogues as potential aromatase inhibitors.
pubmed:publicationType
Journal Article, Research Support, U.S. Gov't, P.H.S., Research Support, Non-U.S. Gov't