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Synthesis and Anticancer Evaluation of New 1,3,4-Oxadiazole Derivatives
- Source :
- Pharmaceuticals, Volume 14, Issue 5, Pharmaceuticals, Vol 14, Iss 438, p 438 (2021)
- Publication Year :
- 2021
- Publisher :
- Multidisciplinary Digital Publishing Institute, 2021.
-
Abstract
- In order to develop novel chemotherapeutic agents with potent anticancer activities, a series of new 2,5-diaryl/heteroaryl-1,3,4-oxadiazoles were designed and synthesized. The structures of the new compounds were established using elemental analyses, IR and NMR spectral data. The compounds were evaluated for their anticancer potential on two standardized human cell lines, HT-29 (colon adenocarcinoma) and MDA-MB-231 (breast adenocarcinoma). Cytotoxicity was measured by MTS assay, while cell cycle arrest and apoptosis assays were conducted using a flow cytometer, the results showing that the cell line MDA-MB-231 is more sensitive to the compounds’ action. The results of the predictive studies using the PASS application and the structural similarity analysis indicated STAT3 and miR-21 as the most probable pharmacological targets for the new compounds. The promising effect of compound 3e, 2-[2-(phenylsulfanylmethyl)phenyl]-5-(4-pyridyl)-1,3,4-oxadiazole, especially on the MDA-MB-231 cell line motivates future studies to improve the anticancer profile and to reduce the toxicological risks. It is worth noting that 3e produced a low toxic effect in the D. magna 24 h assay and the predictive studies on rat acute toxicity suggest a low degree of toxic risks.
- Subjects :
- Mts assay
Cell cycle checkpoint
Structural similarity
mechanism prediction
hydrazide derivatives
Pharmaceutical Science
Pharmacology
Article
03 medical and health sciences
0302 clinical medicine
Pharmacy and materia medica
HT-29 cells
Drug Discovery
MDA-MB-231 cells
Cytotoxicity
nitrogen scaffolds
030304 developmental biology
0303 health sciences
Chemistry
STAT inhibitors
apoptosis induction
Acute toxicity
RS1-441
Cell culture
Apoptosis
030220 oncology & carcinogenesis
cytotoxic agents
Molecular Medicine
Medicine
1 3 4 oxadiazole derivatives
miR-21
Subjects
Details
- Language :
- English
- ISSN :
- 14248247
- Database :
- OpenAIRE
- Journal :
- Pharmaceuticals
- Accession number :
- edsair.doi.dedup.....1fbc7caae236b86ddc2d65af53d987de
- Full Text :
- https://doi.org/10.3390/ph14050438