Rational Design, Synthesis and Biological Evaluation of Pyrimidine-4,6-diamine derivatives as Type-II inhibitors of FLT3 Selective Against c-KIT. [PDF]
FMS-like Tyrosine Kinase 3 (FLT3) is a clinically validated target for acute myeloid leukemia (AML). Inhibitors targeting FLT3 have been evaluated in clinical studies and have exhibited potential to treat FLT3-driven AML.
Bharate, Jaideep B +8 more
core +2 more sources
Heterocycles from cyclopropenones
Great attention has been paid to cyclopropenones as they are present in many natural sources.
Ashraf A. Aly +5 more
openaire +2 more sources
The two β-carbonic anhydrases (CAs, EC 4.2.1.1) from the pathogenic bacterium Brucella suis, BsuCA1 and BsuCA2, were investigated for their inhibition profile with a series of pyridine-3-sulphonamide derivatives incorporating 4-hetaryl moieties.
Simona Maria Monti +5 more
doaj +1 more source
Synthesis and late-stage functionalization of complex molecules through C-H fluorination and nucleophilic aromatic substitution. [PDF]
We report the late-stage functionalization of multisubstituted pyridines and diazines at the position α to nitrogen. By this process, a series of functional groups and substituents bound to the ring through nitrogen, oxygen, sulfur, or carbon are ...
Fier, Patrick S, Hartwig, John F
core +3 more sources
4-Chloro-6-ethoxy-2-(methylthio)pyrimidine
4,6-Dichloro-2-(methylthio)pyrimidine (3) reacts with EtONa in EtOH, at ca. 20 °C, for 2 h, to give exclusively 4-chloro-6-ethoxy-2-(methylthio)pyrimidine (5) in 89% yield. The latter is presented as a useful multifunctionalised pyrimidine scaffold.
Andreas S. Kalogirou +1 more
doaj +1 more source
(E)-3-Heteroarylidenechroman-4-ones as potent and selective monoamine oxidase-B inhibitors [PDF]
A series of (E)-3-heteroarylidenechroman-4-ones (1a-r) was designed, synthesized and investigated in vitro for their ability to inhibit the enzymatic activity of both human monoamine oxidase (hMAO) isoforms, hMAO-A and hMAO-B.
Alcaro, Stefano +6 more
core +1 more source
Aminoazole-Based Diversity-Oriented Synthesis of Heterocycles
The comprehensive review contains the analysis of literature data concerning reactions of heterocyclization of aminoazoles and demonstrates the application of these types of transformations in diversity-oriented synthesis.
Maryna V. Murlykina +7 more
doaj +1 more source
Methods for treating bone deficit conditions with benzothiazole [PDF]
" Compounds containing two aromatic systems covalently linked through a linker containing one or more atoms, or ""linker"" defined as including a covalent bond per se so as to space the aromatic systems at a distance 1.5-15 .ANG., are effective in ...
Baindur, Nand +6 more
core +1 more source
Transformation of (allo)securinine to (allo)norsecurinine via a molecular editing strategy
Securinega alkaloids have intrigued chemists since the isolation of securinine in 1956. This family of natural products comprises a securinane subfamily with a piperidine substructure and norsecurinane alkaloids featuring a pyrrolidine core.
Seoyoung Kim, Hee-Seung Lee, Sunkyu Han
doaj +1 more source
Amine, Amido, and Imido Complexes of Tantalum Supported by a Pyridine-Linked Bis(phenolate) Pincer Ligand: Ta−N π-Bonding Influences Pincer Ligand Geometry [PDF]
A series of tantalum imido and amido complexes supported by a pyridine-linked bis(phenolate) ligand has been synthesized. Characterization of these complexes via X-ray crystallography reveals both C_s and C_2 binding modes of the bis(phenolate)pyridine ...
Bercaw, John E. +3 more
core +2 more sources

