4.3 Article

Facile and expedient synthesis and anti-proliferative activity of diversely pyrrolones bearing 1,3-diphenylpyrazole moiety

Journal

SYNTHETIC COMMUNICATIONS
Volume 50, Issue 2, Pages 185-196

Publisher

TAYLOR & FRANCIS INC
DOI: 10.1080/00397911.2019.1691737

Keywords

Cytotoxic; antitumor; acid hydrazide; pyrrolones; pyrazoles

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A series of some pyrrolone derivatives were synthesized from the acid hydrazide, derived from a pyrazolyl-2(3H)-furanone, through treating with some carbonyl reagents such as 1-phenyl-3-(thiophen-2-yl)-1H-pyrazole-4-carbaldehyde, formic acid, lauroyl chloride, succinoyl chloride, propionic anhydride, as well as, ethoxymethylene malononitrile. All compounds were obtained in good yields and characterized by their microanalytical and spectral data. The synthesized products were evaluated for their in vitro antitumor activity against two human carcinoma cell lines (HCT-116 and MCF7) using doxorubicin as a reference drug by MTT assay. The results revealed that some compounds exhibited significant potency. Noteworthy, the N-propionyl hydrazide derivative was the most potent against both cell lines.

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