Novel pyrazolo[3,4-d]pyrimidines as dual Src-Abl inhibitors active against mutant form of Abl and the leukemia K-562 cell line
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- 作者：Samir M. El-Moghazya ; Riham F. Georgea ; rihamfgeorge@yahoo.com" class="auth_mail" title="E-mail the corresponding author ; Essam Eldin A. Osmana ; Ahmed A. Elbatrawyb ; Miroslava Kissovac ; Ambra Colomboc ; Emmanuele Crespanc ; Giovanni Magac
- 关键词：Pyrazolo[3 ; 4-d]pyrimidines ; Src inhibition ; Abl inhibition ; K-562 cell line ; Molecular modeling
- 刊名：European Journal of Medicinal Chemistry
- 出版年：2016
- 出版时间：10 November 2016
- 年：2016
- 卷：123
- 期：Complete
- 页码：1-13
- 全文大小：2061 K
文摘
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Some pyrazolo[3,4-d]pyrimidines were prepared as dual Src-Abl inhibitors.
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Compounds 7a, 7b revealed good activity against the T315I mutant Abl and Src.
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Compound 10b exerted equal inhibition against both Abl forms.
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10b, The rigide analog of 7b showed a decreased activity against both enzymes.
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These compounds showed promising cytotoxic activity against K-562 cell line.
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