title: Solid-phase synthesis of diamine and polyamine amino acid derivatives as HIV-1 tat-TAR binding inhibitors.
abstract: A series of diamine and polyamine derivatives, either free amines or salts (HCl or TFA), of aspartic and glutamic acid were prepared in excellent yields using Rink Amide solid-phase synthesis. The asparagine and glutamine derivatives were all evaluated for their ability to inhibit Tat-TAR binding using a FIGS cellular assay, with the polyamine derivatives exhibiting the most promising binding activity.
authors.affiliation: Welsh School of Pharmacy, Cardiff University, King Edward VII Avenue, UK.
authors.forename: G
authors.initials: G
authors.lastname: Jimenez Bueno
authors.forename: T
authors.initials: T
authors.lastname: Klimkait
authors.forename: I H
authors.initials: IH
authors.lastname: Gilbert
authors.forename: C
authors.initials: C
authors.lastname: Simons
mesh_terms: D019380:Anti-HIV Agents / Q000138:chemical synthesis / Q000494:pharmacology; D001224:Aspartic Acid / Q000031:analogs & derivatives* / Q000494:pharmacology*; D002459:Cell Fusion; D002460:Cell Line; D004279:DNA, Viral / Q000378:metabolism; D003959:Diamines / Q000138:chemical synthesis* / Q000494:pharmacology; D015696:Gene Products, tat / Q000037:antagonists & inhibitors* / Q000378:metabolism; D018698:Glutamic Acid / Q000031:analogs & derivatives* / Q000494:pharmacology*; D023581:HIV Fusion Inhibitors / Q000494:pharmacology; D016325:HIV Long Terminal Repeat; D015497:HIV-1 / Q000187:drug effects / Q000235:genetics / Q000378:metabolism*; D006367:HeLa Cells; D006801:Humans; D011073:Polyamines / Q000138:chemical synthesis* / Q000494:pharmacology; D013329:Structure-Activity Relationship; D014162:Transfection; D054322:tat Gene Products, Human Immunodeficiency Virus
chemical_list: D019380:Anti-HIV Agents; D004279:DNA, Viral; D003959:Diamines; D015696:Gene Products, tat; D023581:HIV Fusion Inhibitors; D011073:Polyamines; D054322:tat Gene Products, Human Immunodeficiency Virus; D001224:Aspartic Acid; D018698:Glutamic Acid