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Retinoic acid receptor ligands based on the 6-cyclopropyl-2,4-hexadienoic acid
- Source :
- Bioorganicmedicinal chemistry letters. 13(2)
- Publication Year :
- 2002
-
Abstract
- A series of novel cyclopropanyl methyl hexadienoic acid retinoids was designed and prepared. These compounds exhibited either selective activity as RXR agonists or pan-agonists on one or more of each of the RAR and RXR isoforms. The most potent pan-agonist 5a (RAR's EC(50)=17-59 nM; RXR's EC(50)=6-14 nM) showed good antiproliferative properties in the in vitro cancer cell lines, ME 180 and RPMI 8226.
- Subjects :
- Gene isoform
Cyclopropanes
Stereochemistry
medicine.drug_class
Receptors, Retinoic Acid
Carboxylic acid
Clinical Biochemistry
Pharmaceutical Science
Retinoid X receptor
Ligands
Transfection
Biochemistry
Chemical synthesis
Binding, Competitive
Drug Discovery
medicine
Tumor Cells, Cultured
Humans
Retinoid
Molecular Biology
chemistry.chemical_classification
Cell growth
Chemistry
organic chemicals
Organic Chemistry
Biological activity
Cell Differentiation
General Medicine
In vitro
Sorbic Acid
body regions
Retinoic acid receptor
Hexadienoic Acid
embryonic structures
Molecular Medicine
Indicators and Reagents
Cancer cell lines
Cell Division
Subjects
Details
- ISSN :
- 0960894X
- Volume :
- 13
- Issue :
- 2
- Database :
- OpenAIRE
- Journal :
- Bioorganicmedicinal chemistry letters
- Accession number :
- edsair.doi.dedup.....ed8bc78f5625c6e8214435ced5d045ab