4.3 Article

Synthesis and antitumor activity evaluation of some pyrrolone and pyridazinone heterocycles derived from 3-((2-oxo-5-(p-tolyl)furan-3(2H)-ylidene)methyl)quinolin-2(1H)-one

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SYNTHETIC COMMUNICATIONS
卷 50, 期 7, 页码 1046-1055

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TAYLOR & FRANCIS INC
DOI: 10.1080/00397911.2020.1731549

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Cytotoxicity; furanone; pyridazinone; pyrrolone; quinoline

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The broad spectrum of biological activity of quinoline derivatives coupled with our interest in the chemistry of furanones led us to synthesize a quinoline derivative bearing a 2(3H)-furanone scaffold. This derivative was used as a key starting material for the construction of some pyrrolone, imidazole, and pyridazinone derivatives obtained by reactions with some nitrogen nucleophiles viz. ammonium acetate, benzylamine, 1,2-diaminoethane, and hydrazine hydrate. The hydrazide obtained was condensed with 3-chlorobenzaldehyde, 1,3-diphenyl-1H-pyrazole-4-carbaldehyde, isatin, and dodecanoyl chloride to achieve the corresponding hydrazone and pyrrolone derivatives. Also, the synthesized compounds were evaluated for their in vitro antitumor activity using two cancer cell lines: breast and colon tumors. Some compounds displayed satisfactory activities.

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