Tag: M.W=500-550

Hu, Aohan published the artcileChelating the Alpha Therapy Radionuclides ²²⁵Ac³⁺ and ²¹³Bi³⁺ with 18-Membered Macrocyclic Ligands Macrodipa and Py-Macrodipa, Name: 6,6′-((1,4,10,13-Tetraoxa-7,16-diazacyclooctadecane-7,16-diyl)bis(methylene))dipicolinic acid, the publication is Inorganic Chemistry (2022), 61(2), 801-806, database is CAplus and MEDLINE.

The radionuclides ²²⁵Ac³⁺ and ²¹³Bi³⁺ possess favorable phys. properties for targeted alpha therapy (TAT), a therapeutic approach that leverages α radiation to treat cancers. A chelator that effectively binds and retains these radionuclides is required for this application. The development of ligands for this purpose, however, is challenging because the large ionic radii and charge-diffuse nature of these metal ions give rise to weaker metal-ligand interactions. In this study, we evaluated two 18-membered macrocyclic chelators, macrodipa and py-macrodipa, for their ability to complex ²²⁵Ac³⁺ and ²¹³Bi³⁺. Their coordination chem. with Ac³⁺ was probed computationally and with Bi³⁺ exptl. via NMR spectroscopy and X-ray crystallog. Furthermore, radiolabeling studies were conducted, revealing the efficient incorporation of both ²²⁵Ac³⁺ and ²¹³Bi³⁺ by py-macrodipa that matches or surpasses the well-known chelators macropa and DOTA. Incubation in human serum at 37 °C showed that ~90% of the ²²⁵Ac³⁺-py-macrodipa complex dissociates after 1 d. The Bi³⁺-py-macrodipa complex possesses remarkable kinetic inertness reflected by an EDTA transchelation challenge study, surpassing that of Bi³⁺-macropa. This work establishes py-macrodipa as a valuable candidate for ²¹³Bi³⁺ TAT, providing further motivation for its implementation within new radiopharmaceutical agents.

Inorganic Chemistry published new progress about 1128304-86-8. 1128304-86-8 belongs to pyridine-derivatives, auxiliary class Pyridines, name is 6,6′-((1,4,10,13-Tetraoxa-7,16-diazacyclooctadecane-7,16-diyl)bis(methylene))dipicolinic acid, and the molecular formula is C26H36N4O8, Name: 6,6′-((1,4,10,13-Tetraoxa-7,16-diazacyclooctadecane-7,16-diyl)bis(methylene))dipicolinic acid.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem

Thiele, Nikki A. published the artcileAn Eighteen-Membered Macrocyclic Ligand for Actinium-225 Targeted Alpha Therapy, Related Products of pyridine-derivatives, the publication is Angewandte Chemie, International Edition (2017), 56(46), 14712-14717, database is CAplus and MEDLINE.

The 18-membered macrocycle H₂macropa was investigated for ²²⁵Ac chelation in targeted alpha therapy (TAT). Radiolabeling studies showed that macropa, at submicromolar concentration, complexed all ²²⁵Ac (26 kBq) in 5 min at RT. [²²⁵Ac(macropa)]⁺ remained intact over 7 to 8 days when challenged with either excess La³⁺ ions or human serum, and did not accumulate in any organ after 5 h in healthy mice. A bifunctional analog, macropa-NCS, was conjugated to trastuzumab as well as to the prostate-specific membrane antigen-targeting compound RPS-070. Both constructs rapidly radiolabeled ²²⁵Ac in just minutes at RT, and macropa-Tmab retained >99 % of its ²²⁵Ac in human serum after 7 days. In LNCaP xenograft mice, ²²⁵Ac-macropa-RPS-070 was selectively targeted to tumors and did not release free ²²⁵Ac over 96 h. These findings establish macropa to be a highly promising ligand for ²²⁵Ac chelation that will facilitate the clin. development of ²²⁵Ac TAT for the treatment of soft-tissue metastases.

Angewandte Chemie, International Edition published new progress about 1128304-86-8. 1128304-86-8 belongs to pyridine-derivatives, auxiliary class Pyridines, name is 6,6′-((1,4,10,13-Tetraoxa-7,16-diazacyclooctadecane-7,16-diyl)bis(methylene))dipicolinic acid, and the molecular formula is C14H12N2S, Related Products of pyridine-derivatives.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem