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Paper | Regular issue | Vol 91, No. 9, 2015, pp.1735-1751
Published online, 6th August, 2015
DOI: 10.3987/COM-15-13282
Synthesis and in vitro Cytotoxicity Evaluation of New 2-Thioxo-benzo[g]quinazolin-4(3H)-one Derivatives

Rashad Al-Salahi,* Rabab A. El Dib, and Mohamed Marzouk*

*Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh-11451, Saudi Arabia


Preparation of the titled 2-thioxo-benzo[g]quinazolin-4(3H)-ones (1–4) has been previously reported. In the present study, compounds (1–4) were elaborated in high and quantitative yields by simple modification on the reported synthetic route. Treatment of 2-thioxo-benzo[g]quinazolin-4(3H)-ones (1–4) with hydrazine hydrate or with different alkyl(heteroalkyl) halides afforded smoothly the target products 5, 6 or 7–28 in good and high yields. The in vitro cytotoxicity of compounds 1–28 was evaluated against colon HCT-116, hepatocellular Hep-G2, and breast MCF-7, prostate PC-3 and lung A-549 cancer cell lines, using MTT assay. The IC50-values of the target compounds are recorded in µg/mL and doxorubicin used as a reference drug. The results revealed that compounds 1, 3, 7, 10, 13, 14, 15, 16, 20, 21 and 22 had significant cytotoxic effects in relation to the reference drug. The structures of compounds 1–28 were elucidated by means of 1H- and 13C-NMR and HREI mass spectrometry.