Makara Journal of Science
Vol. 27, No. 1

Synthesis and Study of Anticancer and Antioxidant Activities of 2-oxoquinoline Hydrazide Derivatives

Mohamed, Marwa Khalil (Unknown)
Salem, Ezzeldin Mohamed S. (Unknown)
Ali, Ibrahim Ahmed I. (Unknown)



Article Info

Publish Date
25 Mar 2023

Abstract

In this work, hydrazone, thiosemicarbazide, diamide, and dipeptide derivatives were prepared from the glycine and β-alanine hydrazide of 4-hydroxy-2-oxoquinoline. The desired derivative resulted from substitution, hydrazinolysis, condensation, and azide coupling reactions. The fabricated derivatives were screened for anticancer characteristics toward human’s colon carcinoma (HCT-116) cell line using the 3-[4,5-dimethylthiazol-2-yl]-2,5 diphenyl tetrazolium bromide viability assay, while antioxidant property was examined using an in vitro H2O2 scavenging method. The β-alanine hydrazide derivative 3a showed a remarkable IC50 value of 18.8 μg/mL, whereas its corresponding thiosemicarbazide 5b exhibited moderate activeness with an IC50 value of 26.89 μg/mL. Conversely, the dipeptide derivative 7 with a Gly-β-Ala sequence showed better activity than the β-Ala-Gly derivative 8a. The IC50 values of 27.28 and 61.4 μg/mL, respectively, were achieved. According to an H2O2 scavenging activity test, the hydrazide of β-Ala derivative 2a displayed the best H2O2 scavenging property, with an IC50 value of 38.7 μg/mL.

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Journal Info

Abbrev

publication:science

Publisher

Subject

Description

Makara Journal of Science publishes original research or theoretical papers, notes, and minireviews on new knowledge and research or research applications on current issues in basic sciences, namely: Material Sciences (including: physics, biology, and chemistry); Biochemistry, Genetics, and ...