Structure-activity relationships in carboxamide derivatives based on the targeted delivery of radionuclides and boron atoms by means of peripheral benzodiazepine receptor ligands.
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.
Cappelli
Andrea
A
Dipartimento Farmaco Chimico Tecnologico, Università degli Studi di Siena, Via A. Moro, 53100 Siena, Italy. cappelli@unisi.it
Pericot Mohr
Gal la
Gl
Gallelli
Andrea
A
Giuliani
Germano
G
Anzini
Maurizio
M
Vomero
Salvatore
S
Fresta
Massimo
M
Porcu
Patrizia
P
Maciocco
Elisabetta
E
Concas
Alessandra
A
Biggio
Giovanni
G
Donati
Alessandro
A
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
D000577:Amides; D001880:Boranes; D008024:Ligands; D011804:Quinolines; D019275:Radiopharmaceuticals; D011963:Receptors, GABA-A; D011374:Progesterone; D011284:Pregnenolone; D011280:Pregnanolone