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A new series of pyrazolo[3,4-d]pyrimidines has been synthesized. The new compounds were tested for their antitumor activity on 60 different cell lines, and some of the compounds were found to have potent antitumor activity. In particular, 2-hydroxybenzaldehyde [1-(4-chlorophenyl)-3-methyl-1H-pyrazolo-[3,4-d]pyrimidin-4-yl]hydrazone (VIIa) was found to be the most effective among the other derivatives, showing IC50 values of 0.326 to 4.31 μM on 57 different cell lines.

Synthesis of Novel Pyrazolo[3,4-d]pyrimidine Derivatives as Potential anti-BreastCancer Agents. -Novel pyrazolo[3,4-d]pyrimidine derivatives (IV) are synthesized and screened for their cytotoxic activity against the human breast cancer cell line MCF7. Most of these compounds exhibit potent antitumor activity comparable to that of doxorubicin. Compound (IVc) is found to be the most active substance in the series. -(ABD EL HAMID, M. K.; MIHOVILOVIC, M. D.; EL-NASSAN*, H. B.; Eur. J. Med. Chem. 57 (2012) 323-328, http://dx.