Isothiazole dioxides: Synthesis and inhibition of Trypanosoma brucei protein farnesyltransferase
Articolo
Data di Pubblicazione:
2002
Citazione:
Isothiazole dioxides: Synthesis and inhibition of Trypanosoma brucei protein farnesyltransferase / F. Clerici, M.L. Gelmi, K. Yokoyama, D. Pocar, W.C. Van Voorhis, F.S. Buckner, M.H. Gelb. - In: BIOORGANIC & MEDICINAL CHEMISTRY LETTERS. - ISSN 0960-894X. - 12:16(2002), pp. 2217-2220. [10.1016/S0960-894X(02)00338-4]
Abstract:
A series of isothiazole dioxides was synthesized and evaluated as inhibitors of protein farnesyltransferase from the parasite that causes African sleeping sickness (Trypanosoma brucei). The most potent compound in the series inhibited the parasite enzyme with an IC50 of 2 μM and blocked the growth of the bloodstream parasite in vitro with an ED50 of 10 μM. The same compound inhibited rat protein farnesyltransferase and protein geranylgeranyltransferase type I only at much higher concentration. © 2002 Elsevier Science Ltd. All rights reserved.
Tipologia IRIS:
01 - Articolo su periodico
Elenco autori:
F. Clerici, M.L. Gelmi, K. Yokoyama, D. Pocar, W.C. Van Voorhis, F.S. Buckner, M.H. Gelb
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