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Synthesis and anti-metastatic effects of novel chiral ionone alkaloid derivatives
- Source :
- European Journal of Medicinal Chemistry. 101:245-253
- Publication Year :
- 2015
- Publisher :
- Elsevier BV, 2015.
-
Abstract
- Novel chiral ionone alkaloid derivatives were synthesized and evaluated their anti-metastatic effects in human MDA-MB-231 breast cancer cells. The chiral center C-6 of derivatives exerted an important role in response to the anti-metastatic activity. Comparing with a positive control of LY294002, compounds 17b and 19a exhibited potent inhibitory effects on the EGF-induced invasion of MDA-MB-231 cells with IC50 values of 0.026 ± 0.003 and 0.016 ± 0.002 μM, respectively. Moreover, compounds 17b and 19a showed inhibitory effects on the expressions of p-PKCζ and p-integrin β1 in MDA-MB-231 cells in a dose-dependent manner. Thus, compounds 17b and 19a offer potential to be developed as novel anti-metastasis agents.
- Subjects :
- Pharmacology
Dose-Response Relationship, Drug
Molecular Structure
Stereochemistry
Alkaloid
Organic Chemistry
Positive control
Antineoplastic Agents
General Medicine
Inhibitory postsynaptic potential
Ionone
Structure-Activity Relationship
chemistry.chemical_compound
Biochemistry
chemistry
Cell Line, Tumor
Drug Discovery
Ic50 values
Humans
LY294002
Breast cancer cells
Drug Screening Assays, Antitumor
Neoplasm Metastasis
Norisoprenoids
Cell Proliferation
Subjects
Details
- ISSN :
- 02235234
- Volume :
- 101
- Database :
- OpenAIRE
- Journal :
- European Journal of Medicinal Chemistry
- Accession number :
- edsair.doi.dedup.....a916babf32a9abe76c251663362627a7