14401-73-1Relevant articles and documents
A palladium(II)-clipped aromatic sandwich
Kumazawa, Kazuhisa,Yamanoi, Yoshinori,Yoshizawa, Michito,Kusukawa, Takahiro,Fujita, Makoto
, p. 5936 - 5940 (2004)
A filling that makes the sandwich: Large aromatic molecules are sandwiched by two π-conjugated ligands (L) that are joined together by six {(en)Pd} 2+ units (M; en = 1,2-ethanediamine; see picture; guest red, {(en)Pd}2+ yellow, ligand blue). This host has an M6L 2 composition and is distorted by the concave shape of the ligand. Without a guest, it releases the distortion by forming the dimeric M 12L4 in a reversible fashion.
PHENANTHROLINE-TRIAZINE COMPOUND AND ORGANIC LIGHT EMITTING DIODE COMPRISING THE SAME
-
Paragraph 0101; 0103; 0104, (2019/07/03)
The present invention relates to a phenanthroline-triazine compound, capable of improving driving voltage and efficiency, and to an organic light emitting device including the same. The phenanthroline-triazine compound is represented by formula 1 or 2. In the chemical formula 1 or 2, X1, X2, X3 and X4 are independently carbon or nitrogen.COPYRIGHT KIPO 2019
A development of chimeric VEGFR2 TK inhibitor based on two ligand conformers from PDB: 1Y6A complex - Medicinal chemistry consequences of a TKs analysis
Lintnerová, Lucia,García-Caballero, Melissa,Gregáň, Fridrich,Melicher?ík, Milan,Quesada, Ana R.,Dobia?, Juraj,Lác, Ján,Sali?ová, Marta,Bohá?, Andrej
, p. 146 - 159 (2014/01/17)
VEGFR2 is an important mediator of angiogenesis and influences fate of some cancer stem cells. Here we analysed all 34 structures of VEGFR2 TK available from PDB database. From them a complex PDB: 1Y6A has an exceptional AAZ ligand bound to TK in form of two conformers (U- and S-shaped). This observation inspired us to develop three chimeric bispyridyl VEGFR2 inhibitors by combining structural features of both AAZ conformers and/or their relative ligand AAX (PDB: 1Y6B). Our most interesting inhibitor 22SYM has an enzymatic VEGFR2 TK activity (IC50: 15.1 nM) comparable or better to the active compounds from clinical drugs Nexavar and Sutent. 22SYM inhibits growth, migration and tube formation of endothelial cells (EC) and selectively induces EC apoptosis. 22SYM also inhibits in vivo angiogenesis in Zebrafish embryo assay. Additionally to the above results, we proved here that tyrosine kinases in an inactive form possessing Type I inhibitors can adopt both a closed or an opened conformation of kinase A-loop independently on their DFG-out arrangement. We proposed here that an activity of certain Type I inhibitors (e.g. 22SYM-like) in complex with DFG-out TK can be negatively influenced by collisions with a dynamically moving TK A-loop.
CARBOXAMIDE OR SULFONAMIDE SUBSTITUTED THIAZOLES AND RELATED DERIVATIVES AS MODULATORS FOR THE ORPHAN NUCLEAR RECEPTOR ROR[GAMMA]
-
, (2014/01/07)
The invention provides modulators for the orphan nuclear receptor RORy and methods for treating RORy mediated diseases by administering these novel RORy modulators to a human or a mammal in need thereof. Specifically, the present invention provides carboxamide or sulfonamide containing cyclic compounds of Formula (1), (1'), (100), (100'), (200) and (200') and the enantiomers, diastereomers, tautomers, /V-oxides, solvates and pharmaceutically acceptable salts thereof.