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

Authors

Marwa Khalil Mohamed, Suez Canal University, Ismailia 41522, EgyptFollow
Ezzeldin Mohamed S. Salem, Suez Canal University, Ismailia 41522, Egypt
Ibrahim Ahmed I. Ali, Suez Canal University, Ismailia 41522, Egypt

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.

Recommended Citation

Mohamed, Marwa Khalil; Salem, Ezzeldin Mohamed S.; and Ali, Ibrahim Ahmed I. (2023) "Synthesis and Study of Anticancer and Antioxidant Activities of 2-oxoquinoline Hydrazide Derivatives," Makara Journal of Science: Vol. 27: Iss. 1, Article 6.
DOI: 10.7454/mss.v27i1.1495
Available at: https://scholarhub.ui.ac.id/science/vol27/iss1/6