Organic Chemistry Department, Faculty of Pharmacy, Cairo University, Kasr El-Aini street, Cairo 11562, Egypt.
Eur J Med Chem. 2010 Nov;45(11):5286-91. doi: 10.1016/j.ejmech.2010.08.048. Epub 2010 Sep 16.
A series of new 6-arylpyrazolo[3,4-d]pyrimidin-4-ones and 6-alkylpyrazolo[3,4-d]pyrimidin-4-ones were synthesized. Some of the newly synthesized compounds were tested in vitro on human colon tumor cell line (HCT116). Most of the test compounds exploited potent antitumor activity, especially compound 10a which displayed the highest activity among the test compounds with IC(50) equal to 0.47 μg/mL.
合成了一系列新型 6-芳基吡唑并[3,4-d]嘧啶-4-酮和 6-烷基吡唑并[3,4-d]嘧啶-4-酮。部分新合成的化合物在人结肠肿瘤细胞系(HCT116)上进行了体外测试。大多数测试化合物表现出很强的抗肿瘤活性,特别是化合物 10a,其在测试化合物中表现出最高的活性,IC50 为 0.47 μg/mL。