153473-49-5Relevant articles and documents
Indoles and pyridazinoindoles as nonnucleoside analog inhibitors of HIV-1 reverse transcriptase
Font, M.,Monge, A.,Cuartero, A.,Ellorriaga, A.,Martinez-Irujo, J.J.,et al.
, p. 963 - 972 (2007/10/03)
The synthesis and the study of the activity of new indol-2-carboxamides and pyridazinoindoles as inhibitors of HIV-1 reverse transcriptase (RT) are presented.The activity of the compounds synthesized as inhibitors of different types of HIV-1 RT (wild type enzyme and mutant forms P236L, Y181C and P236L/Y181C) was evaluated.The activity of the most active compounds was investigated in the syncytia reduction in vitro assay, in HIV-1IIIB-infected HT4lacZ-1 cells.Their potential cytotoxicity was determined in parallel.Two lead compounds,N-piperazin>-5,6-methylenedioxy indol-2-carboxamide 7q and N-piperazin>-5,6-methylenedioxyindol-2-carboxamide 7s have been identified. - Keywords: indole; nonnucleoside RT inhibitor; syncytia assay; HIV-1IIIBHT4lacZ-1 cells