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Synthesis and evaluation of novel isoxazolyl chalcones as potential anticancer agents
- Source :
- Bioorganic Chemistry. 54:38-43
- Publication Year :
- 2014
- Publisher :
- Elsevier BV, 2014.
-
Abstract
- A series of novel isoxazolyl chalcones were synthesized and evaluated for their activities in vitro against four types of human non-small cell lung cancer cells, including H1792, H157, A549 and Calu-1 cells. The preliminary biological screening showed that compounds 5d and 5f – i exhibited significant cytotoxicity, particularly, compounds 5f and 5h were identified as the most potent anticancer agents with IC 50 values 1.35–2.07 μM and 7.27–11.07 μM against H175, A549 and Calu-1 cell lines, respectively. Compounds 5f–i could induce apoptosis in A549 cells by death receptor 5 (DR5) mediated extrinsic pathways. The preliminary structure–activity relationship study showed that compounds bearing electron withdrawing groups (EWG) at the 2-position of the phenyl ring in Ar group were more effective than those with EWG at 4-position. These results further demonstrated that the scaffolds designed in this work might lead to the discovery of novel anti-lung cancer agents.
- Subjects :
- Stereochemistry
Antineoplastic Agents
Apoptosis
Biochemistry
Structure-Activity Relationship
Chalcones
Drug Discovery
Tumor Cells, Cultured
medicine
Humans
Cytotoxicity
Molecular Biology
Cell Proliferation
A549 cell
Dose-Response Relationship, Drug
Molecular Structure
Chemistry
Cell Cycle
Organic Chemistry
Cancer
Isoxazoles
medicine.disease
In vitro
Cell culture
TNFRSF10B
Non small cell
Drug Screening Assays, Antitumor
Subjects
Details
- ISSN :
- 00452068
- Volume :
- 54
- Database :
- OpenAIRE
- Journal :
- Bioorganic Chemistry
- Accession number :
- edsair.doi.dedup.....5c9e386a483075a634266c5792354988
- Full Text :
- https://doi.org/10.1016/j.bioorg.2014.03.004