73344-98-6

Upstream product

• 124090-10-4 dimethyl (4-nitrobenzyl)propanedioate 
• 7598-70-1 diethyl 2-(4-nitrobenzyl)malonate 
• 100-11-8 1-bromomethyl-4-nitro-benzene 

Downstream Products

• 693785-40-9 2-(4-nitrobenzyl)-1,3-dibromopropane 
• 134439-25-1 2-[(4-nitrophenyl)methyl]propan-1,3-diol bis(4-methylbenzenesulfonate) 
• 1276543-48-6 4,11-N,N'-bis(carbo-tert-butoxymethyl)-16-(4-nitrobenzyl)-1,4,8,11-tetraazabicyclo[6.6.3]heptadecane 
• 1276543-49-7 4,11-bis-(carbo-tert-butoxymethyl)-16-(4-aminobenzyl)-1,4,8,11-tetraazabicyclo[ 6.6.3]heptadecane 
• 1276543-57-7 4,10-bis-(carbo-tert-butoxymethyl)-14-(4-nitrobenzyl)-1,4,7,10-tetraazabicyclo[5. 5.3]pentadecane 
• 1276543-58-8 4,10-bis-(carbo-tert-butoxymethyl)-14-(4-aminobenzyl)-1,4,7,10-tetraazabicyclo[ 5.5.3]pentadecane 
• 1330063-60-9 1-[3-iodo-2-(iodomethyl)propyl]-4-nitrobenzene 
• 1276543-59-9 4,10-bis-(carboxymethyl)-14-(4-aminobenzyl)-1,4,7,10-tetraazabicyclo[5.5.3]pentadecane 
• 1276543-82-8 4,11-bis-(carboxymethyl)-16-(4-(bromoacetamido)benzyl)-1,4,8,11-tetraazabicyclo[6.6.3]heptadecane 
• 1278402-25-7 C₅₂H₇₈N₁₄O₁₂S 
• 1276543-50-0 4,11-bis-(carboxymethyl)-16-(4-aminobenzyl)-1,4,8,11-tetraazabicyclo[6.6.3]heptadecane 
• 1276543-52-2 4,11-N,N'-bis(carboxymethyl)-16-(4-isothiocyanatobenzyl)-1,4,8,11-tetraazabicyclo[6.6.3]heptadecane 
• 134439-26-2 3-(4-nitrobenzyl)1,5-pentanedinitrile 
• 119822-22-9 2-(4'-aminobenzyl)propane-1,3-diamine 

Relevant academic research and scientific papers

RADIO-PHARMACEUTICAL COMPLEXES

The invention provides a method for the formation of a tissue-targeting thorium complex, said method comprising; a) forming an octadentate chelator comprising four hydroxypyridinone (HOPO) moieties, substituted in the N-position with a methyl group, and a

Alpha-emitting complexes

The present invention provides a tissue-targeting complex comprising a tissue targeting moiety, an octadentate hydroxypyridinone-containing ligand and the ion of an alpha-emitting thorium radionuclide. The invention additionally provides therapeutic methods employing such complexes, methods of their production and use, and kits and pharmaceutical compositions comprising such complexes.

RADIO-PHARMACEUTICAL COMPLEXES

The invention provides a method for the formation of a tissue-targeting thorium complex, said method comprising; a) forming an octadentate chelator comprising four hydroxypyridinone (HOPO) moieties, substituted in the N-position with a methyl group, and a

RADIO-PHARMACEUTICAL COMPLEXES

The invention provides a method for the formation of a tissue-targeting thorium complex, said method comprising; a) forming an octadentate chelator comprising four hydroxypyridinone (HOPO) moieties, substituted in the N-position with a C l-C s

An efficient chelator for complexation of thorium-227

We present the synthesis and characterization of a highly efficient thorium chelator, derived from the octadentate hydroxypyridinone class of compounds. The chelator forms extremely stable complexes with fast formation rates in the presence of Th-227 (ambient temperature, 20?min). In addition, mouse biodistribution data are provided which indicate rapid hepatobiliary excretion route of the chelator which, together with low bone uptake, supports the stability of the complex in vivo. The carboxylic acid group may be readily activated for conjugation through the ?-amino groups of lysine residues in biomolecules such as antibodies. This chelator is a critical component of a new class of Targeted Thorium Conjugates (TTCs) currently under development in the field of oncology.

Propylene cross-bridged macrocyclic bifunctional chelator: A new design for facile bioconjugation and robust 64cu complex stability

The first macrocyclic bifunctional chelator incorporating propylene cross-bridge was efficiently synthesized from cyclam in seven steps. After the introduction of an extra functional group for facile conjugation onto the propylene cross-bridge, the two carboxylic acid pendants could contribute to strong coordination of Cu(II) ions, leading to a robust Cu complex. The cyclic RGD peptide conjugate of PCB-TE2A-NCS was prepared and successfully radiolabeled with 64Cu ion. The radiolabeled peptide conjugate was evaluated in vivo through a biodistribution study and animal PET imaging to demonstrate high tumor uptake with low background.

ALPHA-EMITTING COMPLEXES

The present invention provides a tissue-targeting complex comprising a tissue targeting moiety, an octadentate hydroxypyridinone-containing ligand and the ion of an alpha-emitting thorium radionuclide. The invention additionally provides therapeutic methods employing such complexes, methods of their production and use, and kits and pharmaceutical compositions comprising such complexes.

NOVEL TETRA-AZA MACROCYCLIC COMPOUND, METHOD FOR PREPARING SAME, AND USE THEREOF

Provided are a cross-bridged tetraaza macrocyclic compound of a novel structure that can be used, for example, as a contrast agent for diagnostic imaging or a radiopharmaceutical and a method for preparing the same. The disclosed tetraaza macrocyclic comp

Efficient N- and C-functionalisation of cyclam macrocycles utilising bisaminal methodology

An efficient synthesis of C-functionalised cyclam macrocycles that employs bisaminal intermediates and allows N-substitution to be controlled is reported.

DNA-directed alkylating agents. 2. Synthesis and biological activity of platinum complexes linked to 9-anilinoacridine

Two different classes of cis-diaminedichloroplatinum(II) complexes linked to the DNA-intercalating chromophore 9-anilinoacridine have been synthesized and evaluated as DNA-targeted antitumor agents. Two different Pt chelating ligands were investigated (based on 1,2-ethanediamine and 1,3-propanediamine), designed to deliver the Pt in an orientation likely to respectively enhance either intrastrand or interstrand cross-linking. Although both sets of ligands were somewhat unstable under neutral or basic conditions with respect to disproportionation, the corresponding Pt complexes, once prepared, appeared to be quite stable. All the Pt complexes were monitored for purity by TLC, HPLC, and FAB mass spectra, and the mode of Pt coordination was established by 195Pt NMR spectroscopy. The complexes appeared to cause simultaneous platination and intercalative unwinding of plasmid DNA. In vitro studies were carried out with both wild-type and cisplatin-resistant P388 cell lines. Whereas cisplatin itself and the ethylenediamine and 1,3-propanediamine complexes used as standards were about 10-fold less active against the resistant line, the ethylenediamine-linked Pt complexes showed no differential toxicity between the two lines and the propanediamine-linked complexes showed significant differentials (up to 8-fold) in favor of the cisplatin-resistant line. However, these were no greater than those shown by the unplatinated ligands themselves. The majority of the acridine complexes were inactive in vivo against the wild-type P388 leukemia. They were very insoluble, and although a suitable formulation was found, this may have been a factor. It is also possible that these compounds bind in such a way as to direct the Pt away from the major groove.