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

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Abstract

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.

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.

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Authors and Affiliations

  1. Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Cairo University, Giza, Egypt

    MANAL M KANDEEL & SAMEHA M ROSHDY

  2. Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Beni Suef University, Beni Suef, Egypt

    EMAN K A ABDELALL, MOHAMED A ABDELGAWAD & PHOEBE F LAMIE

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  1. MANAL M KANDEEL
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  2. SAMEHA M ROSHDY
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  4. MOHAMED A ABDELGAWAD
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KANDEEL, M.M., ROSHDY, S.M., ABDELALL, E.K.A. et al. Design, synthesis and cytotoxic activity of some novel compounds containing pyrazolo[3,4-d]pyrimidines nucleus. J Chem Sci 125, 1029–1043 (2013). https://doi.org/10.1007/s12039-013-0485-8

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