56136-82-4Relevant academic research and scientific papers
INHIBITORS OF FIBROBLAST GROWTH FACTOR RECEPTOR KINASES
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Paragraph 00151; 00152; 00153, (2021/12/28)
Provided herein are heteroaryl inhibitors of fibroblast growth factor receptor kinases, pharmaceutical compositions comprising said compounds, and methods for using said compounds for the treatment of diseases.
Live-Cell Protein Modification by Boronate-Assisted Hydroxamic Acid Catalysis
Adamson, Christopher,Kajino, Hidetoshi,Kanai, Motomu,Kawashima, Shigehiro A.,Yamatsugu, Kenzo
supporting information, p. 14976 - 14980 (2021/09/29)
Selective methods for introducing protein post-translational modifications (PTMs) within living cells have proven valuable for interrogating their biological function. In contrast to enzymatic methods, abiotic catalysis should offer access to diverse and new-to-nature PTMs. Herein, we report the boronate-assisted hydroxamic acid (BAHA) catalyst system, which comprises a protein ligand, a hydroxamic acid Lewis base, and a diol moiety. In concert with a boronic acid-bearing acyl donor, our catalyst leverages a local molarity effect to promote acyl transfer to a target lysine residue. Our catalyst system employs micromolar reagent concentrations and affords minimal off-target protein reactivity. Critically, BAHA is resistant to glutathione, a metabolite which has hampered many efforts toward abiotic chemistry within living cells. To showcase this methodology, we installed a variety of acyl groups inE. colidihydrofolate reductase expressed within human cells. Our results further establish the well-known boronic acid-diol complexation as abona fidebio-orthogonal reaction with applications in chemical biology and in-cell catalysis.
Compound Shape Effects in Minor Groove Binding Affinity and Specificity for Mixed Sequence DNA
Guo, Pu,Farahat, Abdelbasset A.,Paul, Ananya,Harika, Narinder K.,Boykin, David W.,Wilson, W. David
supporting information, p. 14761 - 14769 (2018/11/02)
AT specific heterocyclic cations that bind in the DNA duplex minor groove have had major successes as cell and nuclear stains and as therapeutic agents which can effectively enter human cells. Expanding the DNA sequence recognition capability of the minor
HETEROCYCLIC KINASE INHIBITORS
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Page/Page column 82, (2016/05/19)
The present disclosure is generally directed to compounds which can inhibit AAK1 (adaptor associated kinase 1), compositions comprising such compounds, and methods for inhibiting AAK1.
Condensed derivatives of imidazole useful as pharmaceuticals
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Paragraph 0634, (2015/09/23)
The invention relates to the compounds (I) and their acids and bases salts: wherein: the dotted line indicates a double bond; X is N or C-R1 and Y is N or C-R2, X and Y not being simultaneously N; A is selected from the group consisting of phenyl, naphthyl and (5-11) membered monocyclic or bicyclic unsaturated cycle or heterocycle possibly substituted as defined in the application, and A can also comprise either a further (4-7) membered heterocycle, said heterocycle being a monocycle, fused, saturated or unsaturated, the polycyclic system then comprising up to 14 members and up to 5 heteroatoms selected from N, O and S; B is Hydrogen or a substituent as defined in the application, or B is a (4-10) membered mono or bicyclic saturated or unsaturated heterocycle containing 1-3 heteroatoms selected from N, O and S, and possibly substituted as defined in the application; B not being Hydrogen when X is N and Y is C-R2; R1 is Hydrogen or a substituent as defined in the application; B and R1 cannot be simultaneously Hydrogen; R2 is Hydrogen or Halogen; their preparation, their use in the antibacterial prevention and therapy, alone or in association with antibacterials, antivirulence agents or drugs reinforcing the host innate immunity, and pharmaceutical compositions and associations containing them.
Optimizing sensitization processes in dinuclear luminescent lanthanide oligomers: Selection of rigid aromatic spacers
Lemonnier, Jean-Francois,Guenee, Laure,Beuchat, Cesar,Wesolowski, Tomasz A.,Mukherjee, Prasun,Waldeck, David H.,Gogick, Kristy A.,Petoud, Stephane,Piguet, Claude
supporting information; experimental part, p. 16219 - 16234 (2011/12/01)
This work illustrates a simple approach for optimizing the lanthanide luminescence in molecular dinuclear lanthanide complexes and identifies a particular multidentate europium complex as the best candidate for further incorporation into polymeric materials. The central phenyl ring in the bis-tridentate model ligands L3-L5, which are substituted with neutral (X = H, L3), electron-withdrawing (X = F, L4), or electron-donating (X = OCH 3, L5) groups, separates the 2,6-bis(benzimidazol-2-yl)pyridine binding units of linear oligomeric multi-tridentate ligand strands that are designed for the complexation of luminescent trivalent lanthanides, Ln(III). Reactions of L3-L5 with [Ln(hfac)3(diglyme)] (hfac- is the hexafluoroacetylacetonate anion) produce saturated single-stranded dumbbell-shaped complexes [Ln2(Lk)(hfac)6] (k = 3-5), in which the lanthanide ions of the two nine-coordinate neutral [N 3Ln(hfac)3] units are separated by 12-14 A. The thermodynamic affinities of [Ln(hfac)3] for the tridentate binding sites in L3-L5 are average (6.6 ≥ log(β2,1Y,Lk) ≥ 8.4) but still result in 15-30% dissociation at millimolar concentrations in acetonitrile. In addition to the empirical solubility trend found in organic solvents (L4 > L3 ? L5), which suggests that the 1,4-difluorophenyl spacer in L4 is preferable, we have developed a novel tool for deciphering the photophysical sensitization processes operating in [Eu2(Lk)(hfac) 6]. A simple interpretation of the complete set of rate constants characterizing the energy migration mechanisms provides straightforward objective criteria for the selection of [Eu2(L4)(hfac)6] as the most promising building block.
Improved synthesis of functionalized mesogenic 2,6-bisbenzimidazolylpyridine ligands
McKenzie, Blayne M.,Miller, Adriane K.,Wojtecki, Rudy J.,Johnson, J. Casey,Burke, Kelly A.,Tzeng, Karis A.,Mather, Patrick T.,Rowan, Stuart J.
, p. 8488 - 8495 (2008/12/20)
A versatile one-pot synthetic platform for the preparation of a range of functionalized 2,6-bisbenzimidazolylpyridine (Bip) derivatives is presented. This protocol significantly reduces the cost and time of previous synthetic routes, while facilitating sc
