H2Me-do2pa: an attractive chelator with fast, stable and inert Bi-nat(3+) and Bi-213(3+) complexation for potential alpha-radioimmunotherapy applications

作者：Lima Luis M P; Beyler Maryline; Oukhatar Fatima; Le Saec Patricia; Faiyre Chauvet Alain; Platas Iglesias Carlos^*; Delgado Rita; Tripier Raphael

来源：Chemical Communications, 2014, 50(82): 12371-12374.

DOI：10.1039/c4cc05529b

The complexation properties of H2Me-do2pa towards Bi-nat(3+) reveal a rather fast formation of the [Bi(Me-do2pa)](+) complex, which is endowed with a very high thermodynamic stability (log K-BiL = 34.2) and presents a single non-fluxional structure in solution. X-ray diffraction and solution NMR studies showed an octadentate binding of the ligand to the metal ion. The labelling of H2Me-do2pa with Bi-213 was performed and the resulting complex was stable in vitro, sustaining its use as an attractive alternative to H(4)dota taken here as a reference.

• 出版日期2014-10-21