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Synthesis and In Vitro Antitumor Activity of New Substituted Thiopyrimidine Acyclic Nucleosides and Their Thioglycoside Analogs
Authors:Wael A. El-Sayed  Aymn E. Rashad  Samir M. Awad  Mamdouh M. Ali
Affiliation:1. Photochemistry Department , National Research Center , El Dokki, Cairo, Egypt;2. Faculty of Pharmacy , Helwan University , Cairo, Egypt;3. Biochemistry Department, Division of Genetic Engineering and Biotechnology , National Research Center , Cairo, Egypt
Abstract:Some new thiopyrimidine acyclic nucleosides and thioglycoside derivatives 3a-c, 4a-c, 6a,b, and 7a,b were synthesized. The cytotoxicity and antitumor evaluation of all prepared compounds have been tested in vitro against Ehrlich's ascites carcinoma cell line and their activity against glutathione peroxidase and catalase were reported. The role of the prepared compounds as free radical regulators and the therapeutic antitumor effect of a balanced generation of free radicals are discussed. Compounds 2, 3b, 3c, 4a, and 4c inhibited significantly in a dose dependent manner the growth of Ehrlich ascites carcinoma cells while the other compounds did not show any antitumor activity even at higher concentrations.
Keywords:Thiopyrmidines  acyclic nucleosides  thioglycosides  free radicals  antitumor activity
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