Events7th International Electronic Conference on Medicinal Chemistry
Published
This submission belongs to the session S4. Fighting cancers of the event 7th International Electronic Conference on Medicinal Chemistry
Published date
03 Nov, 2021
Academic Editor
author-avatarJean Jacques Vanden Eynde
Citation
Camelia Elena Stecoza, George Mihai Nitulescu, Constantin Draghici, Miron Teodor Caproiu, Octavian Tudorel Olaru, Marinela Bostan, Mirela Mihaila, New 1,3,4-oxadiazole derivatives and their role in tumor processes, in Proceedings of 7th International Electronic Conference on Medicinal Chemistry, 1 November–30 November 2021, MDPI: Basel, Switzerland, doi: 10.3390/ECMC2021-11475
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New 1,3,4-oxadiazole derivatives and their role in tumor processes

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Miron Teodor Caproiu 3
1. Carol Davila University of Medicine & Pharmacy, Faculty of Pharmacy, Romania
2. Carol Davila University of Medicine and Pharmacy, Faculty of Pharmacy
3. Costin D. Nenitescu Centre of Organic Chemistry Romanian Academy
4. Center of Immunology, Stefan S. Nicolau, Institute of Virology
Abstract

Cancer is a rapidly growing disease of current era. Continuous research is going on in the direction to develop effective molecules for the treatment of the cancer. The new compounds such as 2,5-diaryl/heteroaryl-1,3,4-oxadiazoles were synthesized and evaluated for anticancer activity. The new 1,3,4-oxadiazole derivatives were obtained by the treatment of aromatic carboxylic acids, with different hydrazide derivatives in the presence of phosphorus oxychloride. Elemental analysis, IR and NMR spectral data confirmed the structures of the compounds. To analyze the antitumor effect of these new compounds, in vitro treatments were performed on two standardized human tumor cell lines, HT-29 (colon adenocarcinoma) and MDA-MB-231 (breast adenocarcinoma), treated with different concentrations of the compounds for different periods of time. The cytotoxic activity of the new compounds was assessed by the colorimetric MTS test. Flow cytometry assay was used to evaluate how compounds influence some processes such as the cell cycle or apoptosis in tumor cells. The analysis of the results shows that the compound with pyridine ring presented the best antitumor profile of the series, probably due to the presence of the pyridine ring next to the oxadiazole structure, acting differently on the two tumor cell lines. The obtained results support the antitumor effect of the analyzed compounds and encourage the extension of the study on other tumor cells in order to improve the anticancer activity and reduce the toxicological risks of the obtained compounds.

Keywords
apoptosis induction
cytotoxic agents
HT-29 cells
MDA-MB-231 cells
oxadiazoles
Poster
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