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4-Hydroxy-6-methoxyaurones with High-Affinity Binding to Cytosolic Domain of P-Glycoprotein
- Source :
- Chemical and Pharmaceutical Bulletin. 50:854-856
- Publication Year :
- 2002
- Publisher :
- Pharmaceutical Society of Japan, 2002.
-
Abstract
- A series of 4-hydroxy-6-methoxyaurones and 4,6-dimethoxyaurones has been synthesised and tested for their binding affinity toward the nucleotide-binding domain of P-glycoprotein, an ABC (ATP-Binding Cassette) transporter which mediates the resistance of cancer cells to chemotherapy. These compounds differ from each other by the nature of the substituent on the aurone B-ring. The binding affinity seems to be linked to the nature of the substituent, as well as to the presence or the absence of a hydroxy group at position 4. The most active compounds were 4'-bromo-4-hydroxy-6-methoxyaurone and 4-hydroxy-4'-iodo-6-methoxyaurone.A series of 4-hydroxy-6-methoxyaurones and 4,6-dimethoxyaurones has been synthesised and tested for their binding affinity toward the nucleotide-binding domain of P-glycoprotein, an ABC (ATP-Binding Cassette) transporter which mediates the resistance of cancer cells to chemotherapy. These compounds differ from each other by the nature of the substituent on the aurone B-ring. The binding affinity seems to be linked to the nature of the substituent, as well as to the presence or the absence of a hydroxy group at position 4. The most active compounds were 4'-bromo-4-hydroxy-6-methoxyaurone and 4-hydroxy-4'-iodo-6-methoxyaurone.
- Subjects :
- Binding Sites
biology
Chemistry
Stereochemistry
Substituent
ATP-binding cassette transporter
Transporter
General Chemistry
General Medicine
Ligand (biochemistry)
Protein Structure, Tertiary
chemistry.chemical_compound
Cytosol
Protein structure
Biochemistry
Drug Resistance, Neoplasm
Drug Discovery
Aurone
[SDV.BBM] Life Sciences [q-bio]/Biochemistry, Molecular Biology
biology.protein
ATP Binding Cassette Transporter, Subfamily B, Member 1
Binding site
Benzofurans
P-glycoprotein
Subjects
Details
- ISSN :
- 13475223 and 00092363
- Volume :
- 50
- Database :
- OpenAIRE
- Journal :
- Chemical and Pharmaceutical Bulletin
- Accession number :
- edsair.doi.dedup.....a30475d51f6e4454665cf10b5026deb0