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Letters in Drug Design & Discovery


ISSN (Print): 1570-1808
ISSN (Online): 1875-628X

Research Article

Design, Synthesis and Cytotoxicity of Novel Coumarin-1,2,3-triazole-1,2,4- Oxadiazole Hybrids as Potent Anti-breast Cancer Agents

Author(s): Maryam Mohammadi-Khanaposhtani, Kiana Fahimi, Elahe Karimpour-Razkenari, Maliheh Safavi, Mohammad Mahdavi, Mina Saeedi and Tahmineh Akbarzadeh*

Volume 16, Issue 7, 2019

Page: [818 - 824] Pages: 7

DOI: 10.2174/1570180815666180627121006

Price: $65


Background: This work reports design, synthesis, and in vitro cytotoxicity of novel coumarin-1,2,3-triazole-1,2,4-oxadiazole hybrids against three breast cancer cell lines MCF-7, MDA-MB-231, and T-47D.

Methods: Synthetic procedure for the preparation of desired compounds was started from the reaction of coumarins or with propargyl bromide to give O-propargylated coumarins or 5. Then, click reaction between the later compounds and 3-aryl-5-(chloromethyl)-1,2,4-oxadiazoles afforded the desired products in good yields.

Results: Among the synthesized compounds, 4-((1-((3-(4-chlorophenyl)-1,2,4-oxadiazol-5- yl)methyl)-1H-1,2,3-triazol-4-yl)methoxy)-2H-chromen-2-one (9a) showed the best cytotoxicity against breast cancer cell lines.

Conclusion: Compound 9a depicted the most activity toward MDA-MB-231 and T-47D cells while compounds 8a and 8c were the most potent compounds against MCF-7.

Keywords: Anti-breast cancer, coumarin, cytotoxicity, 1, 2, 4-oxadiazole, 1, 2, 3-triazole, in vitro.

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