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Synthesis and Biological Evaluation of Amino Chalcone Derivatives as Antiproliferative Agents
- Source :
- Molecules, Volume 25, Issue 23, Molecules, Vol 25, Iss 5530, p 5530 (2020)
- Publication Year :
- 2020
- Publisher :
- Multidisciplinary Digital Publishing Institute, 2020.
-
Abstract
- Chalcone is a common scaffold found in many biologically active compounds. The chalcone scaffold was also frequently utilized to design novel anticancer agents with potent biological efficacy. Aiming to continue the research of effective chalcone derivatives to treat cancers with potent anticancer activity, fourteen amino chalcone derivatives were designed and synthesized. The antiproliferative activity of amino chalcone derivatives was studied in vitro and 5-Fu as a control group. Some of the compounds showed moderate to good activity against three human cancer cells (MGC-803, HCT-116 and MCF-7 cells) and compound 13e displayed the best antiproliferative activity against MGC-803 cells, HCT-116 cells and MCF-7 cells with IC50 values of 1.52 &mu<br />M (MGC-803), 1.83 &mu<br />M (HCT-116) and 2.54 &mu<br />M (MCF-7), respectively which was more potent than the positive control (5-Fu). Further mechanism studies were explored. The results of cell colony formatting assay suggested compound 10e inhibited the colony formation of MGC-803 cells. DAPI fluorescent staining and flow cytometry assay showed compound 13e induced MGC-803 cells apoptosis. Western blotting experiment indicated compound 13e induced cell apoptosis via the extrinsic/intrinsic apoptosis pathway in MGC-803 cells. Therefore, compound 13e might be a valuable lead compound as antiproliferative agents and amino chalcone derivatives worth further effort to improve amino chalcone derivatives&rsquo<br />potency.
- Subjects :
- Chalcone
synthesis
Cell Survival
Cell
Pharmaceutical Science
chalcone
Antineoplastic Agents
Apoptosis
Chemistry Techniques, Synthetic
01 natural sciences
Article
Analytical Chemistry
lcsh:QD241-441
chemistry.chemical_compound
Inhibitory Concentration 50
Structure-Activity Relationship
lcsh:Organic chemistry
antiproliferative
Cell Line, Tumor
Drug Discovery
medicine
Humans
DAPI
Physical and Theoretical Chemistry
Cell Proliferation
Molecular Structure
cell apoptosis
010405 organic chemistry
Organic Chemistry
Intrinsic apoptosis
Biological activity
In vitro
0104 chemical sciences
010404 medicinal & biomolecular chemistry
medicine.anatomical_structure
chemistry
Biochemistry
Chemistry (miscellaneous)
Molecular Medicine
Drug Screening Assays, Antitumor
Lead compound
Subjects
Details
- Language :
- English
- ISSN :
- 14203049
- Database :
- OpenAIRE
- Journal :
- Molecules
- Accession number :
- edsair.doi.dedup.....31c4991d4a92bf2c4cc108982064b5f0
- Full Text :
- https://doi.org/10.3390/molecules25235530