ALK5 kinase inhibitory activity and synthesis of 2,3,4-substituted 5,5-dimethyl-5,6-dihydro-4H-pyrrolo[1,2-b]pyrazoles

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• 作者：Eva Řezn&iacute ; čková ; ^a ; Luká ; &scaron ; Tenora^b ; Pavl&iacute ; na Posp&iacute ; &scaron ; ilová ; ^a ; Juraj Galeta^b ; ¹ ; Radek Jorda^a ; Karel Berka^c ; Pavel Majer^d ; Milan Potá ; ček^b ; Vladim&iacute ; r Kry&scaron ; tof^a ; ^{vladimir.krystof@upol.cz}
• 关键词：Transforming growth factor beta receptor I ; Protein kinase ; Inhibitor ; Substituted pyrrolo[1 ; 2-b]pyrazoles
• 刊名：European Journal of Medicinal Chemistry
• 出版年：2017
• 出版时间：15 February 2017
• 年：2017
• 卷：127
• 期：Complete
• 页码：632-642
• 全文大小：1248 K
• 卷排序：127

文摘

Synthesis of variously substituted 5,5-dimethyl-5,6-dihydro-4H-pyrrolo[1,2-b]pyrazoles. Kinase assays reveal high activity towards ALK5. Mechanism of action in cells corresponds to ALK5 inhibition. Compounds display low cytotoxicity in cell lines.