4-(Aminoalkylamino)-3-benzimidazole-quinolinones as potent CHK-1 inhibitors

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-...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2006-06, Vol.16 (12), p.3121-3124
Hauptverfasser:	Ni, Zhi-Jie, Barsanti, Paul, Brammeier, Nathan, Diebes, Anthony, Poon, Daniel J., Ng, Simon, Pecchi, Sabina, Pfister, Keith, Renhowe, Paul A., Ramurthy, Savithri, Wagman, Allan S., Bussiere, Dirksen E., Le, Vincent, Zhou, Yasheen, Jansen, Johanna M., Ma, Sylvia, Gesner, Thomas G.
Format:	Artikel
Sprache:	eng
Schlagworte:	Alkylation Amination Antineoplastic agents Benzimidazoles - chemistry Biological and medical sciences Cell Line, Tumor Checkpoint Kinase 1 CHK-1 kinase inhibitor Crystallography, X-Ray General aspects Humans Inhibitory Concentration 50 Kinase Medical sciences Models, Molecular Molecular Structure Pharmacology. Drug treatments Protein Kinase Inhibitors - chemical synthesis Protein Kinase Inhibitors - chemistry Protein Kinase Inhibitors - pharmacology Protein Kinases - chemistry Protein Kinases - metabolism Quinolones - chemical synthesis Quinolones - chemistry Quinolones - pharmacology Structure-Activity Relationship Synergy
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Zusammenfassung:	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.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2006.03.059