Tuesday , 5 March 2024

Synthesis and Biological Evaluation of Novel Pyrimidine Derivatives as Potential Anticancer agents

Khalid M.H. Hilmy*a, Mohamed M.M. Solimana, Esmat B.A. Shahinb, Maha M.A. Khalifac
aDepartment of Chemistry, Faculty of Science, Monufyia University, Shebin El-Kom, Egypt.
bDepartment of Biochemistry, Faculty of Medicine for girls, Al-Azahar University, Naser City, Cairo, Egypt.
c Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Al-Azahar University, Naser City, Cairo, Egypt

A new series of novel pyrimidine derivatives (2-30)wereobtained from propylthiouracil (1) and evaluated for antitumour activity. The newly synthesized compounds were characterized by IR, 1HNMR, 13CNMR, MS and elemental analysis. Eight of the synthesized compounds were selected and tested by National Cancer Institute (NCI), USA, for anticancer activity against 60 different human tumour cell lines. Among the compounds tested, 2-(3,5-Dimethyl-1H-pyrazol-1-yl)-6-propyl-3,4-dihydropyrimidin-4-one (26)(NSC 771835)was found to be the most active candidate of the series at fivedose level screening with no selectivity towards any cell panels.
Keywords: Antitumour agents, Pyrimidine derivative, Propylthiouracil, NCI-USA

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