Back to Search
Start Over
Design, synthesis and multidrug resistance reversal activity evaluation of 8-oxocoptisine derivatives.
- Source :
-
Medicinal chemistry (Shariqah (United Arab Emirates)) [Med Chem] 2012 Jul; Vol. 8 (4), pp. 742-8. - Publication Year :
- 2012
-
Abstract
- Fifteen derivatives of 8-oxocoptisine were prepared based on that 8-oxocoptisine showed potent reversing effect against human cancer cells charactering multidrug resistance (MDR). The derivatives were evaluated for their growth inhibition and effects on reversing P-gp-mediated MDR against MCF-7/AMD cells. 12, 13-dinitro-8-oxocoptisine (6c), the most potential candidate with weak growth inhibition, significantly increased the sensitivity of adriamycin (ADM) against MCF-7/ADM cells by 213-fold at 10 μM that was comparable to the reference compound verapamil. The preliminary structure-activity relationships (SARs) of these derivatives were discussed on the basis of the in vitro MDR reversal activities.
- Subjects :
- Antineoplastic Agents chemical synthesis
Berberine chemical synthesis
Berberine chemistry
Berberine pharmacology
Breast Neoplasms drug therapy
Cell Line, Tumor
Cell Proliferation drug effects
Female
Humans
Inhibitory Concentration 50
Molecular Structure
Structure-Activity Relationship
Antineoplastic Agents pharmacology
Berberine analogs & derivatives
Drug Design
Drug Resistance, Multiple drug effects
Drug Resistance, Neoplasm drug effects
Subjects
Details
- Language :
- English
- ISSN :
- 1875-6638
- Volume :
- 8
- Issue :
- 4
- Database :
- MEDLINE
- Journal :
- Medicinal chemistry (Shariqah (United Arab Emirates))
- Publication Type :
- Academic Journal
- Accession number :
- 22548337
- Full Text :
- https://doi.org/10.2174/157340612801216148