947589-65-3Relevant academic research and scientific papers
A new potential approach to block HIV-1 replication via protein-protein interaction and strand-transfer inhibition
Ferro, Stefania,De Luca, Laura,Lo Surdo, Giuseppa,Morreale, Francesca,Christ, Frauke,Debyser, Zeger,Gitto, Rosaria,Chimirri, Alba
, p. 2269 - 2279 (2014/04/17)
Therapeutic treatment of AIDS is recently characterized by a crescent effort towards the identification of multiple ligands able to target different steps of HIV-1 life cycle. Taking into consideration our previously obtained SAR information and combining some important chemical structural features we report herein the synthesis of novel benzyl-indole derivatives as anti-HIV agents. Through this work we identified new dual target small molecules able to inhibit both IN-LEDGF/p75 interaction and the IN strand-transfer step considered as two crucial phases of viral life cycle.
New 4-[(1-benzyl-1H-indol-3-yl)carbonyl]-3-hydroxyfuran-2(5H)-ones, β-diketo acid analogs as HIV-1 integrase inhibitors
Ferro, Stefania,Barreca, Maria Letizia,De Luca, Laura,Rao, Angela,Monforte, Anna Maria,Debyser, Zeger,Witvrouw, Myriam,Chimirri, Alba
, p. 292 - 298 (2008/02/10)
In addition to our recent report on a series of rationally designed benzylindolyldiketo acids acting as potent HIV-1 integrase strand transfer inhibitors, we disclose the results obtained with novel compounds chemically modified on the diketo acid moiety in order to investigate its influence on the biological activity and cytotoxicity. The activity of designed and synthesized 4-[(1-benzyl-1H-indol-3-yl)carbonyl]-3-hydroxyfuran-2(5H)-one derivatives lies in the micromolar range with regard to HIV IN enzymatic activity. The microwave-assisted synthesis was employed in some steps of the chemical procedures.
