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Dadun > Depósito Académico > CIMA (Centro de Investigación Médica Aplicada) > Área de Terapia génica y Hepatología > Inmunología experimental > DA - CIMA - Terapia génica y Hepatología - Inmunología experimental - Artículos de revista >

Synthesis and anti-HIV-1 activities of new pyrimido[5,4-b]indoles
Authors: Merino, I. (Isidro)
Monge, A. (Antonio)
Font, M. (María)
Martinez-de-Irujo, J.J. (Juan José)
Alberdi, E. (Elena)
Santiago, E. (Esteban)
Prieto, I. (Isidro)
Lasarte, J.J. (Juan José)
Sarobe, P. (Pablo)
Borras-Cuesta, F. (Francisco)
Keywords: Pyrimido[5,4-b]indoles
HIV-1 RT inhibitors
HLT4lacZ-1IIIB cells
Issue Date: 1999
Publisher: Elsevier
Publisher version: http://www.sciencedirect.com/science/article/pii/S0014827X9900035X
ISSN: 0014-827X
Citation: I, Monge A, Font M, Martinez de Irujo JJ, Alberdi E, Santiago E, et al. Synthesis and anti-HIV-1 activities of new pyrimido[5,4-b]indoles. Farmaco 1999 Apr 30;54(4):255-264.
Abstract
A set of new pyrimido[5,4-b]indole derivatives that are structurally related to some non-nucleside HIV-1 reverse transcriptase inhibitors were synthesized and biologically evaluated for their activity as inhibitors of wild and mutant HIV-1 RT types in an 'in vitro' recombinant HIV-1 RT screening assay, as well as anti-infectives in HLT4lacZ-1IIIB cells. Preliminary structure-activity relationships suggest that activity is promoted by simultaneous substitution in positions 2 and 4, especially when chains of alkyldiamine type are present, and by electron-releasing substituents (methoxy) in positions 7 and 8. The inactivity or the very low activity of title derivatives does not suggest interest in AIDS therapy.
Permanent link: http://hdl.handle.net/10171/21652
Appears in Collections:DA - Medicina - Medicina Interna - Artículos de revista
DA - CIMA - Terapia génica y Hepatología - Inmunología hepatitis virales - Artículos de revista
DA - CIMA - Terapia génica y Hepatología - Inmunología experimental - Artículos de revista

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