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Synthesis and evaluation of some novel tetrahydropyrimidine derivatives as antimicrobial and cytotoxic agents
Authors:Mogedda E. Haiba  Omar A. Fathalla  Ibrahim F. Zeid  Abdel-mohsen M. Soliman  Sherein I. Abd El-Moez  Walaa S. El-serwy
Affiliation:1. Therapeutical Chemistry Department, National Research Center, Dokki, Cairo, Egypt
2. Pharmacetical Chemistry Department, College of Pharmacy, King Saudi University, Riyadh, 11451, Saudi Arabia
3. Organic Chemistry Department, Faculty of Science, Minufiya University, Shebin El-Kom, Egypt
4. Microbiology and Immunology Department, National Research Center, Dokki, Cairo, Egypt
Abstract:Starting from the reaction of ethyl cyanoacetate with thiourea and the appropriate aldehydes, a series of new thiopyrimidine derivatives were prepared. Antibacterial evaluation results revealed that compounds 12b, 4c and 11b gave the highest antibacterial activity against all tested bacterial strains. Also, some of the novel compounds were evaluated as cytotoxic agents against liver cancer (HEPG2) cell line. It was noticed that some of the derivatives induced significant growth inhibition with IC50 values (ranged from 6.35 to 9.38 μg/mL) in comparison to 5-Fluorouracil after treatment (IC50: 5 μg/mL).
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