{"database":"biostudies-literature","file_versions":[],"scores":null,"additional":{"omics_type":["Unknown"],"volume":["51(15)"],"submitter":["Di Santo R"],"pubmed_abstract":["Novel quinolinonyl diketo acids were designed to obtain integrase (IN) inhibitors selectively active against the strand transfer (ST) step of the HIV integration process. Those new compounds are characterized by a single aryl diketo acid (DKA) chain in comparison to 4, a bifunctional diketo acid reported by our group as an anti-IN agent highly potent against both the 3'-processing and ST steps. Compound 6d was the most potent derivative in IN enzyme assays, while 6i showed the highest potency against HIV-1 in acutely infected cells. The selective inhibition of ST suggested the newly designed monofunctional DKAs bind the IN-DNA acceptor site without affecting the DNA donor site."],"journal":["Journal of medicinal chemistry"],"pagination":["4744-50"],"full_dataset_link":["https://www.ebi.ac.uk/biostudies/studies/S-EPMC2646871"],"repository":["biostudies-literature"],"pubmed_title":["Novel quinolinonyl diketo acid derivatives as HIV-1 integrase inhibitors: design, synthesis, and biological activities."],"pmcid":["PMC2646871"],"pubmed_authors":["Roux A","Marchand C","Crucitti GC","Lavecchia A","Rosi F","Miele G","Galluzzo CM","Andreotti M","Iacovo A","Marinelli L","Novellino E","Palmisano L","Pommier Y","Di Giovanni C","Palamara AT","Costi R","Di Santo R","Amici R","Nencioni L"],"additional_accession":[]},"is_claimable":false,"name":"Novel quinolinonyl diketo acid derivatives as HIV-1 integrase inhibitors: design, synthesis, and biological activities.","description":"Novel quinolinonyl diketo acids were designed to obtain integrase (IN) inhibitors selectively active against the strand transfer (ST) step of the HIV integration process. Those new compounds are characterized by a single aryl diketo acid (DKA) chain in comparison to 4, a bifunctional diketo acid reported by our group as an anti-IN agent highly potent against both the 3'-processing and ST steps. Compound 6d was the most potent derivative in IN enzyme assays, while 6i showed the highest potency against HIV-1 in acutely infected cells. The selective inhibition of ST suggested the newly designed monofunctional DKAs bind the IN-DNA acceptor site without affecting the DNA donor site.","dates":{"release":"2008-01-01T00:00:00Z","publication":"2008 Aug","modification":"2025-04-04T07:58:19.38Z","creation":"2019-03-27T00:20:52Z"},"accession":"S-EPMC2646871","cross_references":{"pubmed":["18646746"],"doi":["10.1021/jm8001422"]}}