914380-10-2Relevant academic research and scientific papers
Novel molecular imaging ligands targeting matrix metalloproteinases 2 and 9 for imaging of unstable atherosclerotic plaques
Hakimzadeh, Nazanin,Pinas, Victorine A.,Molenaar, Ger,De Waard, Vivian,Lutgens, Esther,Van Eck-Smit, Berthe L. F.,De Bruin, Kora,Piek, Jan J.,Eersels, Jos L. H.,Booij, Jan,Verberne, Hein J.,Windhorst, Albert D.
, (2017/12/08)
Molecular imaging of matrix metalloproteinases (MMPs) may allow detection of atherosclerotic lesions vulnerable to rupture. In this study, we develop a novel radiolabelled compound that can target gelatinase MMP subtypes (MMP2/9) with high selectivity and
Design, synthesis and molecular modeling study of iminodiacetyl monohydroxamic acid derivatives as MMP inhibitors
Amelia Santos,Marques, Sergio M.,Tuccinardi, Tiziano,Carelli, Paolo,Panelli, Laura,Rossello, Armando
, p. 7539 - 7550 (2008/02/09)
As the matrix metalloproteinases (MMPs) can be massively up-regulated in degenerative tissues and degrade the extracellular matrix, these key enzymes are promising targets for the therapy of cancer and other degenerative diseases. Here, we are presenting a series of new non-peptidic hydroxamate-based matrix metalloproteinase inhibitors, MMPIs, incorporating the iminodiacetic (IDA) hydroxamic acid scaffold, as mimics of truncated peptidic MMPIs. A series of alkylaryl and sulfonylaryl groups, on the IDA basic scaffold, was investigated with the aim of improving potency and selectivity against MMPs involved in degenerative diseases. The sulfonamide based IDA derivatives studied (compounds B1-B3) showed to be potent (nM range) against deep S1′ pocket MMPs enzymes (i.e., MMP-2).
