DESIGN AND SYNTHESIS OF A NEW-TYPE OF NON STEROIDAL HUMAN AROMATASE INHIBITORS

Authors
SONNET P GUILLON J ENGUEHARD C DALLEMAGNE P BUREAU R RAULT S AUVRAY P MOSLEMI S SOURDAINE P GALOPIN S SERALINI GE
Citation
P. Sonnet et al., DESIGN AND SYNTHESIS OF A NEW-TYPE OF NON STEROIDAL HUMAN AROMATASE INHIBITORS, Bioorganic & medicinal chemistry letters, 8(9), 1998, pp. 1041-1044
Citations number
10
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
8
Issue
9
Year of publication
1998
Pages
1041 - 1044
Database
ISI
SICI code
0960-894X(1998)8:9<1041:DASOAN>2.0.ZU;2-7
Abstract
The structure-activity relationship study of one of recently described aromatase inhibitors, compound 1(MR20814), allowed us to design some related derivatives as potential new inhibitors. Among those we synthe sized, chlorophenylpyridylmethylenetetrahydroinone 5 (MR20492) exhibit ed in vitro a ten-fold higher inhibition of the enzyme (IC50=0.2+/-0.0 mu M and Ki=10.3+/-3.3 nM). (C) 1998 Elsevier Science Ltd. All rights reserved.