Design, Synthesis, and Antitumor Evaluation of Novel Pyrazolo[3,4-d]pyrimidine Derivatives

Manal M. KANDEEL; Lamia W. MOHAMED; Mohammed K. ABD EL HAMID; Ahmed T. NEGMELDIN

doi:10.3797/scipharm.1204-23

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Article

25 June 2012

Design, Synthesis, and Antitumor Evaluation of Novel Pyrazolo[3,4-d]pyrimidine Derivatives

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Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Cairo University, Cairo, Egypt

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Sci. Pharm.2012, 80(3), 531-546;https://doi.org/10.3797/scipharm.1204-23

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Abstract

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.

Keywords:

Pyrazolopyrimidines; Antitumor Activity; Cytotoxic Activity; Synthesis

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