52914-23-5Relevant articles and documents
Structure-activity relationship of a series of diaminoalkyl substituted benzimidazole as neuropeptide Y Y1 receptor antagonists
Zarrinmayeh, Hamideh,Zimmerman, Dennis M.,Cantrell, Buddy E.,Schober, Douglas A.,Bruns, Robert F.,Gackenheimer, Susan L.,Ornstein, Paul L.,Hipskind, Philip A.,Britton, Thomas C.,Gehlert, Donald R.
, p. 647 - 652 (1999)
A series of benzimidazoles (4) was synthesized and evaluated in vitro as potent and selective NPY Y1 receptor antagonists. Substitution of the piperidine nitrogen of 4 with appropriate R groups resulted in compounds with more than 80-fold higher affinity
Iodinated Choline Transport-Targeted Tracers
?vec, Pavel,Novy, Zbyněk,Ku?ka, Jan,Pet?ík, Milo?,Sedlá?ek, Ond?ej,Kucha?, Martin,Li?ková, Barbora,Medvedíková, Martina,Kolouchová, Kristyna,Groborz, Ond?ej,Loukotová, Lenka,Konefa?, Rafa? ?.,Hajdúch, Marián,Hruby, Martin
supporting information, p. 15960 - 15978 (2020/12/23)
We present a novel series of radioiodinated tracers and potential theranostics for diseases accompanied by pathological function of proteins involved in choline transport. Unlike choline analogues labeled with 11C or 18F that are currently used in the clinic, the iodinated compounds described herein are applicable in positron emission tomography, single-photon emission computed tomography, and potentially in therapy, depending on the iodine isotope selection. Moreover, favorable half-lives of iodine isotopes result in much less challenging synthesis by isotope exchange reaction. Six of the described compounds were nanomolar ligands, and the best compound possessed an affinity 100-fold greater than that of choline. Biodistribution data of 125I-labeled ligands in human prostate carcinoma bearing (PC-3) mice revealed two compounds with a biodistribution profile superior to that of [18F]fluorocholine.
Support curvature and conformational freedom control chemical reactivity of immobilized species
Zdobinsky, Tino,Sankar Maiti, Pradipta,Klajn, Rafal
supporting information, p. 2711 - 2714 (2014/03/21)
We show that bimolecular reactions between species confined to the surfaces of nanoparticles can be manipulated by the nature of the linker, as well as by the curvature of the underlying particles.