| Autor: |
Marasco, C. J., Jr., Kramer, D. L., Miller, J., Porter, C. W., Bacchi, C. J., Rattendi, D., Kucera, L., Iyer, N., Bernacki, R., Pera, P., Sufrin, J. R. |
| Zdroj: |
Journal of Medicinal Chemistry; November 2002, Vol. 45 Issue: 23 p5112-5122, 11p |
| Abstrakt: |
A well-defined series of 5-([(Z)-4-amino-2-butenyl]methylamino)-5-deoxyadenosine analogues was designed and synthesized in order to further ascertain the optimal structural requirements for S-adenosylmethionine decarboxylase inhibition and potentially to augment and perhaps separate their antiproliferative and antitrypanosomal activities. Most structural modifications had a deleterious affect on both the antitrypanosomal and antineoplastic activity of 5-([(Z)-4-amino-2-butenyl]methylamino)-5-deoxyadenosine. However, di-O-acetylation of the parent compound produced a potential prodrug that caused markedly pronounced inhibition of trypanosomal and neoplastic cell growth and viability. Moreover, the acetylated derivative of 5-([(Z)-4-amino-2-butenyl]methylamino)-5-deoxyadenosine did inhibit HIV-1 growth and infectivity, whereas the parent compound did not. |
| Databáze: |
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