Abstract
Pyrazolo[3,4-d]pyrimidine analogues were synthesized by treating 3-phenyl-1H-pyrazolo[3,4-d]pyrimidine-4-amine with different sulfonyl chlorides and triethylamine in dry dichloromethane. The structure of all the compounds was elucidated by spectral data and their purity was confirmed by elemental analysis. In vitro antiamoebic activity was performed against HM1:IMSS strain of Entamoeba histolytica and two compounds, 4 (IC50 = 0.57) and 6 (IC50 = 0.68), were found better inhibitors than the reference drug metronidazole (IC50 = 1.80). Further, both the compounds (4 and 6) were low cytotoxic against the human breast cancer MCF-7 cell line in the concentration range of 2.5–250 μM. These preliminary results reveal that pyrazolo[3,4-d]pyrimidine analogues could help in designing better molecules with enhanced antiamoebic activity.
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Siddiqui, S.M., Salahuddin, A. & Azam, A. Pyrazolo[3,4-d]pyrimidine analogues: synthesis, characterization and their in vitro antiamoebic activity. Med Chem Res 22, 775–781 (2013). https://doi.org/10.1007/s00044-012-0070-6
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DOI: https://doi.org/10.1007/s00044-012-0070-6