94347-11-2Relevant articles and documents
Linker Variation and Structure-Activity Relationship Analyses of Carboxylic Acid-based Small Molecule STAT3 Inhibitors
Lopez-Tapia, Francisco,Brotherton-Pleiss, Christine,Yue, Peibin,Murakami, Heide,Costa Araujo, Ana Carolina,Reis Dos Santos, Bruna,Ichinotsubo, Erin,Rabkin, Anna,Shah, Raj,Lantz, Megan,Chen, Suzie,Tius, Marcus A.,Turkson, James
, p. 250 - 255 (2018/03/21)
The molecular determinants for the activities of the reported benzoic acid (SH4-54), salicylic acid (BP-1-102), and benzohydroxamic acid (SH5-07)-based STAT3 inhibitors were investigated to design optimized analogues. All three leads are based on an N-met
Synthesis of bifunctional chelating agents based on mono and diphosphonic derivatives of diethylenetriaminepentaacetic acid
Giovenzana, Giovanni B.,Guanci, Claudia,Demattio, Silvia,Lattuada, Luciano,Vincenzi, Veronica
, p. 4809 - 4813 (2014/06/24)
Bifunctional chelating agents (BFCAs) are small molecules containing a chelating unit, able to strongly coordinate a metal ion, and a reactive functional group, devised to form a stable covalent bond with another molecule. BFCAs are widely employed since their conjugation to a suitable biomolecule (e.g., a peptide or an antibody) allows the synthesis of diagnostic or therapeutic agents that specifically target diseased tissue with metals or radiometals. For this reason, BFCAs find application in diagnostic imaging, molecular imaging, and radiotherapy of cancer. The synthesis of new BFCAs based on a diethylenetriaminepentaacetic acid (DTPA) structure in which one or two carboxylic groups are replaced with phosphonic units is described. The phosphonic group, aside from being a classical isostere of the carboxylic acid in coordination chemistry, allows to modulate the physico-chemical properties of the ligands and of the corresponding complexes.
The in vitro transport of model thiodipeptide prodrugs designed to target the intestinal oligopeptide transporter, PepT1
Foley, David,Pieri, Myrtani,Pettecrew, Rachel,Price, Richard,Miles, Stephen,Lam, Ho Kam,Bailey, Patrick,Meredith, David
supporting information; experimental part, p. 3652 - 3656 (2009/10/23)
A thiodipeptide carrier system is shown to be effective at enabling a range of covalently bound molecules, including benzyl, benzoyl and ibuprofen conjugates, to be transported via the intestinal peptide transporter PepT1, demonstrating its potential as a rational drug delivery target.