Organic Chemistry Department, Faculty of Pharmacy, Cairo University, 33 Kasr El-Aini Street, Cairo 11562, Egypt.
Eur J Med Chem. 2011 Jun;46(6):2031-6. doi: 10.1016/j.ejmech.2011.02.055. Epub 2011 Mar 3.
A series of new pyrido[2,3-d][1,2,4]triazolo[4,3-a]pyrimidines with different substituents at position 3 were synthesized. The effect of the newly synthesized compounds was tested in vitro on human breast adenocarcinoma cell line (MCF7). Some of the synthesized compounds exploited potent antitumor activity, especially the 3-amino derivative 12 which displayed the highest activity among the test compounds with IC50 equal to 3.74 μg/mL.
一系列在 3 位具有不同取代基的新型吡啶并[2,3-d][1,2,4]三唑并[4,3-a]嘧啶被合成出来。新合成的化合物的效果在体外进行了测试，测试对象是人乳腺癌腺癌细胞系（MCF7）。一些合成的化合物表现出了强大的抗肿瘤活性，特别是 3-氨基衍生物 12，其在测试化合物中表现出了最高的活性，IC50 值为 3.74 μg/mL。
