Cell Division Cycle 7 Kinase Inhibitors: 1H-Pyrrolo[2,3-b]pyridines, Synthesis and Structure−Activity Relationships

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• 作者：Antonella Ermoli ; Alberto Bargiotti ; Maria Gabriella Brasca ; Antonella Ciavolella ; Nicoletta Colombo ; Gabriele Fachin ; Antonella Isacchi ; Maria Menichincheri ; Antonio Molinari ; Alessia Montagnoli ; Ant
• 刊名：Journal of Medicinal Chemistry
• 出版年：2009
• 出版时间：July 23, 2009
• 年：2009
• 卷：52
• 期：14
• 页码：4380-4390
• 全文大小：916K
• 年卷期：v.52,no.14(July 23, 2009)
• ISSN：1520-4804

文摘

Cdc7 kinase has recently emerged as an attractive target for cancer therapy and low-molecular-weight inhibitors of Cdc7 kinase have been found to be effective in the inhibition of tumor growth in animal models. In this paper, we describe synthesis and structure−activity relationships of new 1H-pyrrolo[2,3-b]pyridine derivatives identified as inhibitors of Cdc7 kinase. Progress from (Z)-2-phenyl-5-(1H-pyrrolo[2,3-b]pyridin-3-ylmethylene)-3,5-dihydro-4H-imidazol-4-one (1) to [(Z)-2-(benzylamino)-5-(1H-pyrrolo[2,3-b]pyridin-3-ylmethylene)-1,3-thiazol-4(5H)-one] (42), a potent ATP mimetic inhibitor of Cdc7 kinase with IC₅₀ value of 7 nM, is also reported.