title: Structure-activity relationships in carboxamide derivatives based on the targeted delivery of radionuclides and boron atoms by means of peripheral benzodiazepine receptor ligands.
abstract: The structure-activity relationship studies on 2-quinolinecarboxamide peripheral benzodiazepine receptor (PBR) ligands have been refined with the aim of using these ligands as carriers of radionuclides and boron atoms. Some new ligands show enhanced affinity and steroidogenic activity with respect to reference compound 1 and are interesting candidates for radiolabeling and PET studies. Moreover, carborane derivative 3q, representing the first example of PBR ligand bearing a carborane cage, can be useful to explore an alternative mechanism in BNCT.
authors.affiliation: Dipartimento Farmaco Chimico Tecnologico, Università degli Studi di Siena, Via A. Moro, 53100 Siena, Italy. cappelli@unisi.it
authors.forename: Andrea
authors.initials: A
authors.lastname: Cappelli
authors.forename: Gal la
authors.initials: Gl
authors.lastname: Pericot Mohr
authors.forename: Andrea
authors.initials: A
authors.lastname: Gallelli
authors.forename: Germano
authors.initials: G
authors.lastname: Giuliani
authors.forename: Maurizio
authors.initials: M
authors.lastname: Anzini
authors.forename: Salvatore
authors.initials: S
authors.lastname: Vomero
authors.forename: Massimo
authors.initials: M
authors.lastname: Fresta
authors.forename: Patrizia
authors.initials: P
authors.lastname: Porcu
authors.forename: Elisabetta
authors.initials: E
authors.lastname: Maciocco
authors.forename: Alessandra
authors.initials: A
authors.lastname: Concas
authors.forename: Giovanni
authors.initials: G
authors.lastname: Biggio
authors.forename: Alessandro
authors.initials: A
authors.lastname: Donati
mesh_terms: D000577:Amides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D000818:Animals; D001880:Boranes / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D002540:Cerebral Cortex / Q000187:drug effects / Q000378:metabolism; D066298:In Vitro Techniques; D008024:Ligands; D011280:Pregnanolone / Q000096:biosynthesis; D011284:Pregnenolone / Q000096:biosynthesis; D011374:Progesterone / Q000096:biosynthesis; D011804:Quinolines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D011869:Radioligand Assay; D019275:Radiopharmaceuticals / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D051381:Rats; D011963:Receptors, GABA-A / Q000187:drug effects*; D013329:Structure-Activity Relationship
chemical_list: D000577:Amides; D001880:Boranes; D008024:Ligands; D011804:Quinolines; D019275:Radiopharmaceuticals; D011963:Receptors, GABA-A; D011374:Progesterone; D011284:Pregnenolone; D011280:Pregnanolone