Journal of Chemical Sciences

, Volume 125, Issue 5, pp 1029–1043 | Cite as

Design, synthesis and cytotoxic activity of some novel compounds containing pyrazolo[3,4-d]pyrimidines nucleus

  • PHOEBE F LAMIEEmail author


Novel pyrazolo[3,4-d]pyrimidines were designed and synthesized as antitumour agents against human breast cancer adenoma (MCF-7). Molecular modelling and pharmacological screening were performed against breast cancer cell line and also certain synthetic pathways were developed in order to introduce functionality onto C6 and N5 positions of pyrimidine moiety. Surprisingly, all the test compounds showed IC50 lower than that of the standard olomoucine I, especially compounds 4b, 8a, 10b, 11a and b, which showed IC50 between 0.009 and 0.004 \(\upmu \)M.

Graphical Abstract

Compounds with substitution on 1, 5 and 6 sites of pyrazolo [3,4-d] pyrimidinones were synthesized to match the action of cyclin-dependent kinases (CDK) inhibitors. The newly synthesized compounds were evaluated in vitro for their anticancer activity. There was some sort of consistency between modelling study and results of anticancer screening.


Pyrazolo[3,4-d]pyrimidine derivatives cytotoxic activity MCF-7 cyclin-dependent kinase inhibitors (CDKI) 


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© Indian Academy of Sciences 2013

Authors and Affiliations

    • 1
    • 1
    • 2
    • 2
    • 2
    Email author
  1. 1.Pharmaceutical Organic Chemistry Department, Faculty of PharmacyCairo UniversityGizaEgypt
  2. 2.Pharmaceutical Organic Chemistry Department, Faculty of PharmacyBeni Suef UniversityBeni SuefEgypt

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