Synthesis and In-vitro Biological Analyses of New quinazolin-2,4-dione Derivatives

Rashdan, H.R.M.; Okasha, H.; Abdelhakeem, M. A.; Mosallam, A. M.; Temairk, H.; Alhamzani, A.G.; Abou-Krisha, M.M.; Yousef, T.A.; Abdelmonsef, A.H.

doi:10.21608/ejchem.2022.111820.5077

Synthesis and In-vitro Biological Analyses of New quinazolin-2,4-dione Derivatives

Document Type : Original Article

Authors

¹ Chemistry of Natural and Microbial Products Department, Pharmaceutical and Drug Industries Research Institute, National Research Institute, Dokki, Cairo 12622, Egypt.

² Biochemistry and Molecular Biology Department, Theodor Bilharz Research Institute, Giza, Egypt.

³ Chemistry Department, Faculty of Science, South Valley University, 83523 Qena, Egypt.

⁴ Chemistry Department, College of Science, Imam Mohammad Ibn Saud Islamic University (IMSIU), Riyadh 11623, Saudi Arabia.

⁵ Department of Toxic and Narcotic drug, Forensic Medicine, Mansoura Laboratory, Medicolegal organization, Ministry of Justice, Egypt.

10.21608/ejchem.2022.111820.5077

Abstract

A series of quinazolin-2,4-dione analogues (1-17a,b) were prepared and their chemical structures were confirmed using spectral and microanalytical data. Analysis of the in vitro cytotoxic effect of the synthesized compounds using RBCs toxicity assay was achieved. Also, biological screening on their potential anticancer effect on hepatocellular carcinoma cell line (HepG2) and their antimicrobial activity against three microbes (bacteria, yeast, and fungus) was studied. Only two compounds 5 and 17b had a moderate anti-HCC activity with calculated IC50 equals 382.9±6.9 µg/ml and 415.8±3.8 µg/ml, respectively. Compound 9 had the highest anti-Aspergillus niger effect, compound 5 had the highest anti-Candida albicans effect, compound 6 had the highest anti-Staphylococcus aureus effect, and compound

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