111584-10-2Relevant articles and documents
2,6-BIS(((1H-BENZO[D]IMIDAZOL-2-YL)THIO)METHYL)PYRIDINE AND N2,N6-DIBENZYLPYRIDINE-2,6-DICARBOXAMIDE DERIVATIVES AND RELATED COMPOUNDS AS PHOSPHOINOSITIDE 3-KINASE (PI3K) INHIBITORS FOR TREATING CANCER
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Paragraph 127-129, (2020/03/15)
2,6-bis(((lH-benzo[d]imidazol-2-yl)thio)methyl)pyridine and N2, N6-dibenzylpyridine-2, 6-dicarboxamide derivatives and related compounds as phosphoinositide 3-kinase (PI3K) inhibitors for treating cancer. The present invention relates to pharmaceutically active 2,6- bis(((lH-benzo[d]imidazol-2-yl)thio)methyl)pyridine, N2,N6- dibenzylpyridine-2, 6-dicarboxamide and N2,N6-bis(3-hydroxyphenyl) pyridine-2, 6-dicarboxamide, as well as to derivatives thereof, and to structurally related compounds. These compounds are phosphoinositide 3-kinase inhibitors (PI3K) and useful in treating or preventing cancerous diseases. The invention further relates methods of manufacturing such compounds as well as to pharmaceutical compositions and formulations comprising such compounds, optionally together with other pharmaceutically active compounds. The invention further relates to a method for determining the activity of PI3Kalpha or PI3Kalpha mutants, which method includes: a) providing a solid phase which is functionalized by immobilization of GST-GRPl-molecules onto the solid phase, b) performing a PI3Kalpha or PI3Kalpha mutant catalyzed enzyme reaction to convert PIP2 to PIP3, c) adding competitor PIP3 carrying a detectable label or reporter molecule, and d) determining enzyme activity based on the amount of PIP3 obtained in step b) which competes with competitor PIP3 for binding to the functionalized solid phase.
Towards phosphine-free Pd(II) pincer complexes for catalyzing Suzuki-Miyaura cross-coupling reaction in aqueous medium
Jerome, Peter,Sathishkumar, Pushpanathan N.,Bhuvanesh, Nattamai S.P.,Karvembu, Ramasamy
supporting information, p. 115 - 124 (2017/07/22)
Pincer complexes can act as efficient catalysts for many industrially important organic transformations under environmentally benign and mild conditions. The NNN pincer ligands have been prepared from the reactions between pyridine-2,6-dicarbonyldichloride and benzylamine or its derivatives in the presence of 4-dimethylaminopyridine (DMAP). Pd(II) complexes containing NNN pincer ligand and acetonitrile/triphenylphosphine have been synthesized and characterized by analytical, spectroscopic (FT-IR, UV-Visible, 1H, 13C & 31P NMR and Mass) and single crystal X-ray diffraction techniques. Single crystal X-ray analysis reveals a distorted square planar geometry around Pd in all the complexes. These pincer complexes have been used as catalysts in Suzuki-Miyaura cross-coupling reaction. The effect of ancillary ligands (CH3CN and PPh3) in the complexes has been investigated towards the coupling reaction. The conversions have been determined from GC analyses. Scope of the system has been extended with various substituted halides.
Monometallic lanthanide complexes with tridentate 2,6-dicarboxamidopyridine ligands. Influence of peripheral substitutions on steric congestion and antenna effect
Borgne, Thierry Le,Benech, Jean-Marc,Floquet, Sebastien,Bernardinelli, Gerald,Aliprandini, Christian,Bettens, Philippe,Piquet, Claude
, p. 3856 - 3868 (2007/10/03)
The systematic investigation of steric and electronic effects on the formation of lanthanide complexes with the tridentate N,N,N',N'-tetraalkylpyridine-2,6-dicarboxamide ONO ligands (alkyl = ethyl: L5, isopropyl: L6 and benzyl: L7) shows a reduced affinity with incrasing steric demand in the order L5 3+ and [Ln(Li)2]3+ are formed with the three ligands, but 1 : 3 complexes are strictly limited to [Ln(L5)3]3+ and [Ln(L6)3]3+ because of the significant steric congestion provided by the twelve benzyl groups located along the three-fold axis in [Ln(L7)3]3+. Comparisons between L6 and L7 in the 1 : 2 complexes evidence superimposable pseudo-monocapped square antiprismatic coordination spheres in the crystal structures of [Ln(Li)2(H2O)2(CF3SO3)](CF3SO3)2 (i = 6, Ln = Eu: 9, i = 7, Ln = Gd: 10). Photophysical properties of [Ln(L6)2]3+ (Ln = Eu, Gd, Tb, Lu) are similar except for improved quantum yields for [Ln(L7)2]3+ (Ln = Eu, Tb) which can be assigned to a slightly more efficient L7 -> LnIII energy transfer process. The removal of two benzyl groups in the analogous N,N'-dibenzylpyridine-2,6-dicarboxamide ligand (L8) restores the formation of stable triple-helical complexes as demonstrated by the crystal structure of [Tb(L8)3]2(CF3SO3)6 (11). However, the existence of intricate mixtures of isomers in solution which are blocked on the NMR time scale limits their use as building blocks for the design of polymetallic d-f and f-f helicates.
