407-91-0Relevant articles and documents
Heparin-polynitroxides: Synthesis and preliminary evaluation as cardiovascular EPR/MR imaging probes and extracellular space-targeted antioxidants
Kleschyov, Andrei L.,Sen', Vasily,Golubev, Valery,Münnemann, Kerstin,Hinderberger, Dariush,Lackner, Karl J.,Weber, Stefan,Terekhov, Maxim,Schreiber, Laura M.,Münzel, Thomas
, p. 265 - 271 (2012)
We report here the synthesis of heparin-polynitroxide derivatives (HPNs) in which nitroxide moieties are linked either to uronic acid or glycosamine residues of the heparin macromolecule. HPNs have low anticoagulant activity, possess superoxide scavenging
Novel Polyamine-Naphthalene Diimide Conjugates Targeting Histone Deacetylases and DNA for Cancer Phenotype Reprogramming
Pasini, Alice,Marchetti, Chiara,Sissi, Claudia,Cortesi, Marilisa,Giordano, Emanuele,Minarini, Anna,Milelli, Andrea
supporting information, p. 1218 - 1223 (2017/12/26)
A series of hybrid compounds was designed to target histone deacetylases and ds-/G-quadruplex DNAs by merging structural features deriving from Scriptaid and compound 1. Compound 6 binds different DNA arrangements, inhibits HDACs both in vitro and in cells, and is able to induce a reduction of cell proliferation. Moreover, compound 6 displays cell phenotype-reprogramming properties since it prevents the epithelial to mesenchymal transition in cancer cells, inducing a less aggressive and migratory phenotype, which is one of the goals of present innovative strategies in cancer therapies.
A two-step strategy to radiolabel choline phospholipids with99mTc in S180 cell membranes via strain-promoted cyclooctyne–azide cycloaddition reaction
Chen, Qingxin,Chu, Taiwei
supporting information, p. 5472 - 5475 (2016/11/09)
As tumor markers, the radiolabeling of choline (Cho)-containing phospholipids in cellular membranes with99mTc is a challenge. The conventional strategy to combine the metallic radionuclide with Cho by large ligand damages the bioactivity of Cho, resulting in low tumor-to-nontumor ratios. Pretargeting strategy based on strain-promoted cyclooctyne–azide cycloaddition (SPAAC) reaction was applied to solve this general problem. Functional click synthons were synthesized as pretargeting components: azidoethyl-choline (AECho) serves as tumor marker and azadibenzocyclooctyne (ADIBO) conjugated to bis(2-pieolyl) amine (BPA) ligand (ADIBO-BPA) as99mTc(CO)3-labeling and azido-binding group. Both in vitro cell experiment and in vivo biodistribution experiment indicate that it is versatile to radiolabel Cho in cellular membranes via this two-step pretargeting strategy. We believe that this pretargeting strategy can indeed enhance the target-specificity and also reduce background signals to optimize imaging quality.
