Synthesis and biological activity of N-aryl-2-aminothiazoles: potent pan inhibitors of cyclin-dependent kinases
In: Bioorganic & medicinal chemistry letters (Print), Jg. 14 (2004), Heft 11, S. 2973-2977
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Zugriff:
N-Aryl aminothiazoles 6-9 were prepared from 2-bromothiazole 5 and found to be CDK inhibitors. In cells they act as potent cytotoxic agents. Selectivity for CDK1, CDK2, and CDK4 was dependent of the nature of the N-aryl group and distinct from the CDK2 selective N-acyl analogues. The N-2-pyridyl analogues 7 and 19 showed pan CDK inhibitory activity. Elaborated analogues 19 and 23 exhibited anticancer activity in mice against P388 murine leukemia. The solid-state structure of 7 bound to CDK2 shows a similar binding mode to the N-acyl analogues.
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Synthesis and biological activity of N-aryl-2-aminothiazoles: potent pan inhibitors of cyclin-dependent kinases
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| Autor/in / Beteiligte Person: | MISRA, Raj N ; XIAO, Hai-Yun ; KIMBALL, S. David ; LEE, Francis Y ; WEBSTER, Kevin R ; WILLIAMS, David K ; KIM, Kyoung S ; SONGFENG, LU ; KELLER, Kristen A ; MULHERON, Janet G ; BATORSKY, Roberta ; TOKARSKI, John S ; SACK, John S |
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| Zeitschrift: | Bioorganic & medicinal chemistry letters (Print), Jg. 14 (2004), Heft 11, S. 2973-2977 |
| Veröffentlichung: | Oxford: Elsevier, 2004 |
| Medientyp: | academicJournal |
| Umfang: | print, |
| ISSN: | 0960-894X (print) |
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