Document Type : Original Article
Authors
1
Applied Organic Chemistry Department, National Research Centre, Dokki, Cairo, Egypt.
2
Applied organic chemistry, National Research Center
3
Department of Applied Organic Chemistry, Industrial Chemical Division, National Research Center, Cairo, Dokki 12622, Egypt
4
Applied Organic Chem, NRC
5
Applied Organic Chemistry Department, National Research Center, Cairo, Dokki, 12622, Egypt
6
Photochemistry Department, National Research Centre
7
hormones department, medical research division, National research center
8
Department of Cancer Biology, Pharmacology Unit, National Cancer Institute, Cairo University, Cairo 11796, Egypt
9
Photochemistry Department, Naional Research Centre, Dokki, Cairo, Egypt
Abstract
Novel substituted [1,2,3]triazolo[4,5-d]pyrimidine-7-one derivatives were synthesized using 1,2,3-triazolo-4-carboxamide derivative (2) by the reaction with carbon disulfide, triethoxymethane, 4-fluorobenzaldehyde and ethyl benzoate respectively. The S-glucoside, N-glycoside derivatives and acyclic sugar analogs of new synthesized [1,2,3]triazolo[4,5-d]pyrimidines were also synthesized. The synthesized compounds were tested for cytotoxicity and in vitro anticancer activity versus human lung (A549), colon (HCT116) and breast (MCF-7) cancer cell lines. The results disclosed that the synthesized compounds apply their activities in A549 and MCF-7. MCF-7 cells are more sensitive to the tested compounds than the other cell lines. Compounds 2, 3, 9 and 10 exposed promising anticancer activities compared to the action of the ordinarily used anticancer drug, doxorubicin in both A549 and MCF-7 cell lines. A good binding affinities for compounds 2, 3, 6, 10 and 11 were noted in docking studies. Results showed a clear effect of N3-substitution in pyrimidine ring on the activities of the synthesized compounds
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