5-Substituted 3-isopropyl-7-[4-(2-pyridyl)benzyl]amino-1(2)H-pyrazolo[4,3-d]pyrimidines with anti-proliferative activity as potent and selective inhibitors of cyclin-dependent kinases
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- 作者：Ladislava Vymětalová ; a ; Libor Havlí ; čekb ; Antoní ; n &Scaron ; turca ; Zuzana Skrá ; &scaron ; ková ; a ; Radek Jordaa ; Tomá ; &scaron ; Pospí ; &scaron ; ila ; Miroslav Strnada ; Vladimí ; r Kry&scaron ; tofa ; vladimir.krystof@upol.cz" class="auth_mail" title="E-mail the corresponding author
- 关键词：Cyclin-dependent kinase ; Inhibitor ; Selectivity ; Bioisostere
- 刊名：European Journal of Medicinal Chemistry
- 出版年：2016
- 出版时间：3 March 2016
- 年：2016
- 卷：110
- 期：Complete
- 页码：291-301
- 全文大小：1147 K
文摘
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Synthesis of pyrazolo[4,3-d]pyrimidines with nanomolar CDK-inhibitory activity.
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Preliminary kinase profiling of 5b reveals high selectivity for CDK2 and 5.
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Compounds display cytostatic and pro-apoptotic effects.
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Mechanism of action in cells corresponds to CDK inhibition.