Synthesis and anti-HIV-1 activities of new pyrimido[5,4-b]indoles
Keywords: 
Pyrimido[5,4-b]indoles
HIV-1 RT inhibitors
HLT4lacZ-1IIIB cells
Issue Date: 
1999
Publisher: 
Elsevier
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.

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