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Design, Synthesis and Anticancer Evaluation of Substituted Cinnamic Acid Bearing 2-Quinolone Hybrid Derivatives.

ABSTRACT: A new series of hybrid molecules containing cinnamic acid and 2-quinolinone derivatives were designed and synthesized. Their structures were confirmed by 1H-NMR, 13C-NMR and mass analyses. All the synthesized hybrid molecules were assessed for their in vitro antiproliferative activity against more than one cancer cell lines. Compound 3-(3,5-dibromo-7,8-dihydroxy-4-methyl-2-oxoquinolin-1(2H)-ylamino)-3-phenylacrylic acid (5a) with IC50 = 1.89 μM against HCT-116 was proved to the most potent compound in this study, as compared to standard drug staurosporin. DNA flow cytometry assay of compound 5a revealed G2/M phase arrest and pre-G1 apoptosis. Annexin V-FITC showed that the percentage of early and late apoptosis was increased. The results of topoisomerase enzyme inhibition activity showed that the hybrid molecule 5a displays potent inhibitory activity compared with control.

SUBMITTER: Abu Almaaty AH 

PROVIDER: S-EPMC8400797 | biostudies-literature | 2021 Aug

REPOSITORIES: biostudies-literature

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Design, Synthesis and Anticancer Evaluation of Substituted Cinnamic Acid Bearing 2-Quinolone Hybrid Derivatives.

Abu Almaaty Ali H AH   Elgrahy Nermeen A NA   Fayad Eman E   Abu Ali Ola A OA   Mahdy Ahmed R E ARE   Barakat Lamiaa A A LAA   El Behery Mohammed M  

Molecules (Basel, Switzerland) 20210804 16

A new series of hybrid molecules containing cinnamic acid and 2-quinolinone derivatives were designed and synthesized. Their structures were confirmed by <sup>1</sup>H-NMR, <sup>13</sup>C-NMR and mass analyses. All the synthesized hybrid molecules were assessed for their in vitro antiproliferative activity against more than one cancer cell lines. Compound 3-(3,5-dibromo-7,8-dihydroxy-4-methyl-2-oxoquinolin-1(2<i>H</i>)-ylamino)-3-phenylacrylic acid (<b>5a</b>) with IC<sub>50</sub> = 1.89 μM agai  ...[more]

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