A new bis-tetradentate acyclic amine ligand L-Et has been synthesized from 4,6-bis(aminomethyl)-2-phenylpyrimidine and 2-vinylpyridine. Dinuclear complexes, (Mn2LEt)-L-II(MeCN)(H2O)(3)(ClO4)(4) (1), (Fe2LEt)-L-II(H2O)(4)(BF4)(4) (2), (Co2LEt)-L-II(H2O)(3)(MeCN)(2)(...
However, because of the strong paramagnetism of Fe2+ and the weak binding of Fe2+ to the ligand, traditional fluorescent probes have weak metal-selective or only off-type fluorescence response modes, a phenomenon that does not indicate accurately detect and recognize Fe2+ [33], [34], [35]....
First, the effects of SB1518 on ligand-dependent JAK2 signaling in human cell lines endogenously expressing the wild-type JAK2 were examined. Cognate binding of the interferon-g receptors in these cells causes autophosphorylation of JAK2 on Y1007/8 and activation of different STAT proteins depending...
Compound (15) was co-crystallized with Aurora kinase A, and the key ligand–protein interactions were identified. The furopyrimidine core ring formed two hydrogen bonds with Ala 213 and Glu211 residues in the hinge region. Another hydrogen bond was found to be formed between the hydroxyl group...
Adenosine triphosphate (ATP) is an endogenous ligand that is widely distributed throughout the human body. ATP is involved in numerous functions, including cell growth, hearth rhythm, immune function, sleep regulation and angiogenesis. Though there are four subtypes of adenosine receptor, only A2AR ...
Rational design of 1-D metal–organic frameworks based on the novel pyrimidine-4,6-dicarboxylate ligand. New insights into pyrimidine through magnetic inte... Single crystal X-ray analysis of compounds H2pmdc·2H2O (1), KHpmdc (2), and K2pmdc (3) shows that the pyrimidine-4,6-dicarboxyla...
Surprisingly, attempts to crystallize CdLCl 2 from EtOH/Me 2CO mixture afforded single crystals of a compound, having 1:2 metal-to-ligand stoichiometry, CdL 2Cl 2·0.5Me 2CO·1.5H 2O, instead of a complex with 1:1 stoichiometry. At the same time, crystallization of CdL 2Cl 2 from Me...
Preclinical Imaging Evaluation of Novel TSPO-PET Ligand 2-(5,7-Diethyl-2-(4-(2-[18F]fluoroethoxy)phenyl)pyrazolo[1,5-a]pyrim... Purpose Translocator protein (TSPO) concentrations are elevated in glioma, suggesting a role for TSPO positron emission tomography (PET) imaging in this se... ...
A fragment-based lead discovery approach wasused to generate potent and selective MAP4K4 inhibitors. The fragmenthit pursued in this article had excellent ligand efficiency (LE),an important attribute for subsequent successful optimization intodrug-like lead compounds. The optimization efforts eventually ...
However, displaying a high ligand efficiency, these low molecular weight structures can be further optimized to produce new CSF1R inhibitors with improved metabolic stability and cell‐based potencies. Experimental Section General Procedure A: Negishi cross‐coupling: Preparation of benzylzinc bromides: ...