180608-78-0Relevant articles and documents
A versatile acid-labile linker for antibody-drug conjugates
Finniss, Mathew C.,Chu, Kevin S.,Bowerman, Charles J.,Luft, J. Christopher,Haroon, Zishan A.,Desimone, Joseph M.
, p. 1355 - 1358 (2014)
Antibody drug conjugates (ADC) couple therapeutic monoclonal antibodies (mAb) with potent toxins through a linker that is stable within systemic circulation, but cleaves within the target cells. In this report, silyl ether chemistry was used to couple the mAb trastuzumab with the chemotherapeutic, gemcitabine, to demonstrate the use of silyl ethers as a potential linker for ADCs.
SULFAMIDE LINKER, CONJUGATES THEREOF, AND METHODS OF PREPARATION
-
Page/Page column 98, (2016/04/26)
The present invention relates to a compound comprising an alpha-end and an omega-end, the compound comprising on the alpha-end a reactive group Qlcapable of reacting with a functional group F1present on a biomolecule and on the omega-end a target molecule, the compound further comprising a group according to formula (1) or a salt thereof: Said compound may also be referred to as a linker-conjugate. The invention also relates to a process for the preparation of a bioconjugate, the process comprising the step of reacting a reactive group Q1of a linker-conjugate according to the invention with a functional group F1of a biomolecule. The invention further relates to a bioconjugate obtainable by the process according to the invention. In a preferred embodiment, the invention concerns a process for the preparation of a bioconjugate via a cycloaddition, such as a (4+2)-cycloaddition (e.g. a Diels-Alder reaction) or a (3+2)-cycloaddition (e.g. a 1,3-dipolar cycloaddition).
Functionalized phosphonated half-cage molecules as ligands for metal complexes
Villemin, Elise,Herent, Marie-France,Marchand-Brynaert, Jacqueline
supporting information, p. 6165 - 6178 (2013/01/15)
Phosphonated molecules, featuring a half-cage structure and a N-lateral chain with additional metal coordinating groups were designed as ligands of metal cations. These compounds were synthesized by a Diels-Alder (DA) strategy, using 1-diethoxyphosphoryl-1,3-butadiene and a series of N-substituted maleimides as dienophiles. Two cycloadducts, bearing a terminal primary alcohol and a terminal iodide, respectively, were used as key intermediates for further functionalizations. Metal coordination properties of the ligands equipped with functionalized N-lateral chains were proven by an ESI-HRMS study. The stoichiometry of one selected EuIII complex with a diphosphonated ligand was determined by photoluminescence spectroscopy in emission mode.