PMID- 17188490
OWN - NLM
STAT- MEDLINE
DCOM- 20070413
LR  - 20070205
IS  - 0960-894X (Print)
IS  - 0960-894X (Linking)
VI  - 17
IP  - 4
DP  - 2007 Feb 15
TI  - ERbeta ligands. Part 5: synthesis and structure-activity relationships of a 
      series of 4'-hydroxyphenyl-aryl-carbaldehyde oxime derivatives.
PG  - 902-6
AB  - A series of 4'-hydroxyphenyl-aryl-carbaldehyde oximes (5b) was prepared and found 
      to have high affinity (4nM) and modest selectivity (39-fold) for estrogen 
      receptor-beta (ERbeta). Substitution of one of the core rings of the scaffold 
      based around these novel ligands further expanded our knowledge in the quest 
      toward achieving high affinity and selectivity for ERbeta. An X-ray co-crystal of 
      structure 11 revealed that the oxime moiety was mimicking the C-ring of 
      genistein, as previously predicted by SAR and docking studies.
FAU - Mewshaw, Richard E
AU  - Mewshaw RE
AD  - Chemical and Screening Sciences, Wyeth Research, 500 Arcola Road, Collegeville, 
      PA 19426, USA. mewshar@wyeth.com
FAU - Bowen, S Marc
AU  - Bowen SM
FAU - Harris, Heather A
AU  - Harris HA
FAU - Xu, Zhang B
AU  - Xu ZB
FAU - Manas, Eric S
AU  - Manas ES
FAU - Cohn, Stephen T
AU  - Cohn ST
LA  - eng
PT  - Journal Article
DEP - 20061201
PL  - England
TA  - Bioorg Med Chem Lett
JT  - Bioorganic & medicinal chemistry letters
JID - 9107377
RN  - 0 (Aldehydes)
RN  - 0 (Estrogen Receptor beta)
RN  - 0 (Indicators and Reagents)
RN  - 0 (Ligands)
RN  - 0 (Oximes)
RN  - 0 (Selective Estrogen Receptor Modulators)
SB  - IM
MH  - Aldehydes/*chemical synthesis/*pharmacology
MH  - Crystallography, X-Ray
MH  - Estrogen Receptor beta/*drug effects
MH  - Humans
MH  - Indicators and Reagents
MH  - Ligands
MH  - Models, Molecular
MH  - Oximes/*chemical synthesis/*pharmacology
MH  - Selective Estrogen Receptor Modulators/*chemical synthesis/*pharmacology
MH  - Structure-Activity Relationship
EDAT- 2006/12/26 09:00
MHDA- 2007/04/17 09:00
CRDT- 2006/12/26 09:00
PHST- 2006/10/11 00:00 [received]
PHST- 2006/11/13 00:00 [revised]
PHST- 2006/11/20 00:00 [accepted]
PHST- 2006/12/26 09:00 [pubmed]
PHST- 2007/04/17 09:00 [medline]
PHST- 2006/12/26 09:00 [entrez]
AID - S0960-894X(06)01354-0 [pii]
AID - 10.1016/j.bmcl.2006.11.066 [doi]
PST - ppublish
SO  - Bioorg Med Chem Lett. 2007 Feb 15;17(4):902-6. doi: 10.1016/j.bmcl.2006.11.066. 
      Epub 2006 Dec 1.