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Novel compounds with potent CDK9 inhibitory activity for the treatment of myeloma
Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2018-01-02 , DOI: 10.1016/j.bmcl.2018.01.002 Zsófia Czudor 1 , Mária Balogh 2 , Péter Bánhegyi 2 , Sándor Boros 2 , Nóra Breza 2 , Judit Dobos 2 , Márk Fábián 1 , Zoltán Horváth 2 , Eszter Illyés 2 , Péter Markó 2 , Anna Sipos 2 , Csaba Szántai-Kis 2 , Bálint Szokol 2 , László Őrfi 3
中文翻译：
具有有效 CDK9 抑制活性的治疗骨髓瘤的新型化合物
更新日期：2018-01-02
Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2018-01-02 , DOI: 10.1016/j.bmcl.2018.01.002 Zsófia Czudor 1 , Mária Balogh 2 , Péter Bánhegyi 2 , Sándor Boros 2 , Nóra Breza 2 , Judit Dobos 2 , Márk Fábián 1 , Zoltán Horváth 2 , Eszter Illyés 2 , Péter Markó 2 , Anna Sipos 2 , Csaba Szántai-Kis 2 , Bálint Szokol 2 , László Őrfi 3
Affiliation
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Cyclin-dependent kinases (CDKs) and Polo-like kinases (PLKs) play key role in the regulation of the cell cycle. The aim of our study was originally the further development of our recently discovered polo-like kinase 1 (PLK1) inhibitors. A series of new 2,4-disubstituted pyrimidine derivatives were synthesized around the original hit, but their PLK1 inhibitory activity was very poor. However the novel compounds showed nanomolar CDK9 inhibitory activity and very good antiproliferative effect on multiple myeloma cell lines (RPMI-8226).
中文翻译：
具有有效 CDK9 抑制活性的治疗骨髓瘤的新型化合物
细胞周期蛋白依赖性激酶 (CDK) 和 Polo 样激酶 (PLK) 在细胞周期的调节中发挥着关键作用。我们研究的最初目的是进一步开发我们最近发现的 polo 样激酶 1 (PLK1) 抑制剂。围绕原点合成了一系列新的2,4-二取代嘧啶衍生物，但它们的PLK1抑制活性很差。然而，这些新化合物对多发性骨髓瘤细胞系（RPMI-8226）表现出纳摩尔级的 CDK9 抑制活性和非常好的抗增殖作用。
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