4-(Aminoalkylamino)-3-benzimidazole-quinolinones as potent CHK-1 inhibitors
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- 作者：Zhi-Jie Ni ; Paul Barsanti ; Nathan Brammeier ; Anthony Diebes ; Daniel J. Poon ; Simon Ng ; Sabina Pecchi ; Keith Pfister ; Paul A. Renhowe ; Savithri Ramurthy et al.
- 关键词：CHK-1 kinase inhibitor ; Kinase ; Synergy
- 刊名：Bioorganic and Medicinal Chemistry Letters
- 出版年：2006
- 出版时间：15 June 2006
- 年：2006
- 卷：16
- 期：12
- 页码：3121-3124
- 全文大小：155 K
文摘
CHK-1 is one of the key enzymes regulating checkpoints in cellular growth cycles. Novel 4-(amino-alkylamino)-3-benzimidazole-quinolinones were prepared and assayed for their ability to inhibit CHK-1. These compounds are potent cell permeable CHK-1 inhibitors and showed synergistic effect with a DNA-damaging agent, camptothecin.