Efficient synthesis and evaluation of bimodal ligand NETA.

Bioorg Med Chem Lett

Chemistry Division, Biological, Chemical, and Physical Sciences Department, Illinois Institute of Technology, 3101 S. Dearborn Street, LS 182, Chicago, IL 60616, USA.

Published: June 2008

The efficient and short synthetic route to the structurally novel bimodal ligand NETA for antibody-targeted radiation therapy (radioimmunotherapy, RIT) of cancer was developed. The structure of NETA was determined by X-ray crystallography. The arsenazo-based UV spectroscopic complexation kinetics data suggest that NETA is a promising chelator for use in RIT applications of (212)Bi, (213)Bi, and (177)Lu.

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.bmcl.2008.03.084DOI Listing

Publication Analysis

Top Keywords

bimodal ligand
8
ligand neta
8
efficient synthesis
4
synthesis evaluation
4
evaluation bimodal
4
neta
4
neta efficient
4
efficient short
4
short synthetic
4
synthetic route
4

Similar Publications

Macrophage (Mph) polarization and functional activity play an important role in the development of inflammatory lung conditions. The previously widely used bimodal classification of Mph into M1 and M2 does not adequately reflect the full range of changes in polarization and functional diversity observed in Mph in response to various stimuli and disease states. Here, we have developed a model for the direct assessment of Mph from bronchial alveolar lavage fluid (BALF) functional alterations, in terms of phagocytosis activity, depending on external stimuli, such as exposure to a range of bacteria (, and ).

View Article and Find Full Text PDF

Achieving Linear α-Macro-olefins in Ethylene Polymerization through Precisely Tuned Bis(imino)pyridylcobalt Precatalysts with Steric and Electronic Parameters.

Precis Chem

December 2024

Key Laboratory of Engineering Plastics and Beijing National Laboratory for Molecular Science, Institute of Chemistry, Chinese Academy of Sciences, Beijing 100190, China.

Synthesis of functional polyethylene from ethylene alone is tricky and heavily dependent on both the type and structure of the precatalyst and the choice of cocatalyst used in the polymerization. In the present study, a series of cobalt precatalysts was prepared and investigated for ethylene polymerization under various conditions. By incorporation of strong electron-withdrawing groups (F and NO) and a steric component (benzhydryl) into the parent bis(imino)pyridine ligand, the catalytic performance of these precatalysts was optimized.

View Article and Find Full Text PDF

Bronchial asthma remains a serious medical problem, as approximately 10% of patients fail to achieve adequate symptom control with available treatment options. Macrophages play a pivotal role in the pathophysiology of asthma, as well as in some other respiratory disorders. Typically, they are classified into two major classes, M1 and M2; however, recent findings have indicated that in fact there is a whole range of macrophage polarization and functional diversity beyond this bimodal division.

View Article and Find Full Text PDF

In the drug discovery process, accurate prediction of drug-target interactions is crucial to accelerate the development of new drugs. However, existing methods still face many challenges in dealing with complex biomolecular interactions. To this end, we propose a new deep learning framework that combines the structural information and sequence features of proteins to provide comprehensive feature representation through bimodal fusion.

View Article and Find Full Text PDF

A comparative study of the copolymerization of racemic propylene oxide (PO) with CO catalyzed by racemic (salcy)CoX (salcy = ,'-bis(3,5-di--butylsalicylidene)-1,2-diaminocyclohexane; X = perfluorobenzoate (OBzF) or 2,4-dinitrophenoxy (DNP)) in the presence of a [PPN]Cl ([PPN] = bis(triphenylphosphine)iminium) cocatalyst is performed in bulk at 21 °C and a 2.5 MPa pressure of CO. The increase in the nucleophilicity of an attacking anion results in the increase in the copolymerization rate.

View Article and Find Full Text PDF

Want AI Summaries of new PubMed Abstracts delivered to your In-box?

Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!