Synthesis and antitumor activity of some new pyrazolo[1,5-a] pyrimidines |
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| Authors: | Ashraf S. Hassan Mohamed F. Mady Hanem M. Awad Taghrid S. Hafez |
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| Affiliation: | a Department of Organometallic and Organometalloid Chemistry, National Research Centre, Dokki 12622, Cairo, Egypt;b Department of Green Chemistry, National Research Centre, Dokki 12622, Cairo, Egypt;c Department of Mathematics and Natural Science, Faculty of Science and Technology, University of Stavanger, N-4036 Stavanger, Norway;d Department of Tanning Materials and Leather Technology, National Research Centre, Dokki 12622, Cairo, Egypt |
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| Abstract: | New series of pyrazolo[1,5-a]pyrimidine derivatives 7a-i, 11a-c and Schiff bases 13a-c were synthesized and screened for their in vitro antitumor activity against three human carcinoma cell lines, namely colorectal carcinoma (HCT116), prostate adenocarcinoma (PC-3) and liver carcinoma (HepG-2) using MTT cytotoxicity assay at 100 μg/mL. Some of the tested compounds displayed good anticancer activities against HCT-116 and PC-3 cells. Whereas, compounds 7d and 11a showed better antitumor activity than the rest of the compounds against both cell lines. A structure-activity relationship (SAR) has been discussed and structures of the newly synthesized compounds were confirmed by different spectral data (MS, IR, 1H NMR and 13C NMR) and elemental analysis. |
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| Keywords: | 5-Amino-1H-pyrazole Pyrazolo[1 5-a]pyrimidine Schiff bases MTT assay Anticancer activity Structure activity relationship |
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