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

Journal of Chemical Sciences

Mohamed A Abdelgawad¹  Sameha M Roshdy²  Eman K A Abdelall¹  Manal M Kandeel²  Phoebe F Lamie2¹ 

[1] Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Beni Suef University, Beni Suef, Egypt$$;Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Cairo University, Giza, Egypt$$

关键词: Pyrazolo[3;    4-𝑑]pyrimidine derivatives;    cytotoxic activity;    MCF-7;    cyclin-dependent kinase inhibitors (CDKI).;   

DOI  :  

来源: Indian Academy of Sciences

【 摘 要 】

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 𝜇M.

【 授权许可】

Unknown