| Autor: |
Luzzio, F. A., Mayorov, A. V., Ng, S. S. W., Kruger, E. A., Figg, W. D. |
| Zdroj: |
Journal of Medicinal Chemistry; August 2003, Vol. 46 Issue: 18 p3793-3799, 7p |
| Abstrakt: |
Versatile synthesis of the teratogenic, TNFα-modulatory, and antiangiogenic thalidomide analogue 2-(2,6-dioxopiperidine-3-yl)phthalimidine (1) and its direct antiangiogenic properties are described. With thalidomide or thalidomide derivatives as precursors, the synthesis involved either carbonyl reduction/thiation-desulfurization or carbonyl reduction/acyliminium ion reduction protocols. Compared to earlier studies with thalidomide, which was only active with microsomal treatment, 1 exhibited marginal inhibitory activity in the rat aortic ring assay, thereby demonstrating the requirement for metabolic activation. |
| Databáze: |
Supplemental Index |
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