148258-03-1Relevant articles and documents
Synthesis of a coumarin-based europium complex for bioanalyte labeling
Feau, Clementine,Klein, Emmanuel,Kerth, Paul,Lebeau, Luc
, p. 1499 - 1503 (2007)
A coumarin-based europium chelate ready-to-use for analyte labeling and homogeneous time-resolved fluorescence measurements has been designed. Compound 1 displays three functional elements: an azide reactive spacer arm, a coumarin sensitizer, and a seven-coordinate europium complex. That complex can be excited at 370 nm by inexpensive UV-LEDs as a light excitation source.
Efficient Synthesis of a Family of Bifunctional Chelators Based on the PCTA[12] Macrocycle Suitable for Bioconjugation
Leygue, Nadine,Enel, Morgane,Diallo, Abdel,Mestre-Voegtlé, Béatrice,Galaup, Chantal,Picard, Claude
, p. 2899 - 2913 (2019/05/15)
PCTA[12] is a 12-membered tetraaza-macrocyclic ligand that incorporates a pyridine unit within the macrocyclic ring and three acetate pendant arms. Unlike DOTA and NOTA chelators, PCTA is a recent entry to the field of macrocyclic polyaminocarboxylate ligands available to complex a variety of M2+/M3+ ions for biomedical applications such as diagnostic and radiotherapeutic. Despite the promising properties of its chelates, only a few of bifunctional chelating agents (BFCAs) derived from PCTA have been described so far. Based on our very recent methodology for the preparation of PCTA[12] itself, we report here the efficient synthesis of several BFCAs derived from PCTA bearing a free reactive function group, mainly devoted to conjugation purposes: ester, carboxylic acid, alcohol, aliphatic amine, aromatic amine, maleimide, bromo or azide functions. These functions were introduced either on the 4-position of the pyridine ring or on the methylene carbon atom of the central acetate chelating arm, while keeping the three carboxylate groups available for metal chelation. Moreover, two of these BFCAs-PCTA were used for conjugation with a tetrapeptide (cholecystokinin analogue), a bioactive molecule (biotin), or a solid support (silica gel).
COMPOUNDS AND METHODS FOR INHIBITING HISTONE DEMETHYLASES
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Paragraph 00704, (2016/03/22)
The present application relates to compounds being of Formula (I), (II), (III), (IV), (V), (VI), (Ilia), (Illb), (IIIc), (Hid), (Hie), (Illf), and (Illg). Compounds of Formula (I) have the structure: wherein Q, R1, R18, R19, M, A and Y are as defined herein. The compounds of the application can modulate the activity of histone demethylases (HDMEs), and can be useful for the prevention and/or treatment of diseases in which genomic dysregulation is involved in the pathogenesis, e.g., cancer.