新型吡唑并[3,4-d]嘧啶作为双Src-Abl抑制剂，对Abl突变形式和白血病K-562细胞系具有活性。
Novel pyrazolo[3,4-d]pyrimidines as dual Src-Abl inhibitors active against mutant form of Abl and the leukemia K-562 cell line.
作者信息
El-Moghazy Samir M, George Riham F, Osman Essam Eldin A, Elbatrawy Ahmed A, Kissova Miroslava, Colombo Ambra, Crespan Emmanuele, Maga Giovanni
机构信息
Pharmaceutical Chemistry Department, Faculty of Pharmacy, Cairo University, El-kasr Elaini Street, Cairo 11562, Egypt.
Pharmaceutical Chemistry Department, Faculty of Pharmacy, Cairo University, El-kasr Elaini Street, Cairo 11562, Egypt.
出版信息
Eur J Med Chem. 2016 Nov 10;123:1-13. doi: 10.1016/j.ejmech.2016.07.034. Epub 2016 Jul 19.
Some novel 6-substituted pyrazolo[3,4-d]pyrimidines 4, 5, 6a-d, 7a-c, 8 and pyrazolo[4,3-e][1,2,4]triazolo[4,3-a]pyrimidines 9a-c, 10a-c, 11, 12a,b, 13a-c and 14 were synthesized and characterized by spectral and elemental analyses. They were screened for their biological activity in vitro against Abl and Src kinases. Compounds 7a and 7b revealed the highest activity against both wild and mutant Abl kinases as well as the Src kinase and the leukemia K-562 cell line. They can be considered as new hits for further structural optimization to obtain better activity.
合成了一些新型的6-取代吡唑并[3,4-d]嘧啶4、5、6a-d、7a-c、8以及吡唑并[4,3-e][1,2,4]三唑并[4,3-a]嘧啶9a-c、10a-c、11、12a、b、13a-c和14，并通过光谱和元素分析对其进行了表征。对它们针对Abl和Src激酶的体外生物活性进行了筛选。化合物7a和7b对野生型和突变型Abl激酶以及Src激酶和白血病K-562细胞系均显示出最高活性。它们可被视为进一步进行结构优化以获得更好活性的新先导化合物。
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