239093-19-7Relevant academic research and scientific papers
Synthesis and anti-HIV-1 activities of new pyrimido[5,4-b]indoles
Merino, Isidro,Monge, Antonio,Font, Maria,Martinez De Irujo, Juan Jose,Alberdi, Elena,Santiago, Esteban,Prieto, Isidro,Lasarte, Juan Jose,Sarobe, Pablo,Borras, Francisco
, p. 255 - 264 (1999)
A set of new pyrimido[5,4-b]indole derivatives that are structurally related to some non-nucleoside 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-1(IIIB) 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.
