90965-06-3Relevant articles and documents
Unveiling novel 2-cyclopropyl-3-ethynyl-4-(4-fluorophenyl)quinolines as GPCR ligands via PI3-kinase/PAR-1 antagonism and platelet aggregation valuations; development of a new class of anticancer drugs with thrombolytic effects
Thangarasu,Thamarai Selvi,Manikandan
, p. 468 - 480 (2018)
In the present study, novel 2-cyclopropyl-3-ethynyl-4-(4-fluorophenyl) quinolines (4a-l) were recognized and evaluated as G-Protein Coupled Receptor (GPCR) ligands through molecular evaluations. Thrombin mediates adhesion of mast cell, a type of cell abundantly found in connective tissue and releasing histamine and other substances during inflammatory and allergic reactions, through phosphoinositol 3-kinase pathway. With this background, as preliminary, 4a-l are resolute to be potential leads, designated from their effective phosphoinositol 3-kinase (PI3-Kinase) inhibition potentials, best-docked scores, comparative ligand efficiency, and significant structural attributes evaluated by ab initio simulations. Since thrombin is one of the main reason for various cancer invasion in association with PI3Kinase, a thrombolytic potential of the compounds also analyzed. The experimental in vitro studies confirmed the significant enhancement as PI3Kinase inhibitors and appreciable enhancement in MTT assay of breast and skin cancer cell lines. Significantly, acetophenone substituent in the quinoline scaffold could be coherent to note the significant binding affinity to all the evaluated drug targets.
Self-organizing oligothiophene-nucleoside conjugates: Versatile synthesis via "Click"-chemistry
Jatsch, Anja,Kopyshev, Alexey,Mena-Osteritz, Elena,Baeuerle, Peter
, p. 961 - 964 (2008)
A versatile synthesis of novel oligothiophene-nucleoside conjugates based on Cu(l)-catalyzed alkyne-azide cycloaddition ("click-reaction") has been developed. Complementary thymidine- and adenosine-functionalized quaterthiophenes form recognition-driven superstructures via hydrogen bonding and other competing intermolecular forces. Self-aggregated fibers up to 30 μm in length were characterized with atomic force microscopy.
Application of FSO2N3 in preparation of diazo reagent
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Paragraph 0111-0119, (2021/06/06)
The invention discloses application of FSO2N3 in preparation of a diazo reagent. The application comprises the following step: in the presence of alkali, FSO2N3 and acetone dimethyl phosphate as shown in a formula 2 are subjected to a reaction as shown in the specification, and a Bestmann-Ohira and/or Seyferth-Gilbert reagent is obtained. According to the application, the Seyferth-Gilbert reagent and/or the Bestmann-Ohira reagent can be obtained at a high yield in half an hour, the two mixed reagents generated in the reaction do not need to be separated, and the one-pot method is directly applied to the synthesis of the terminal alkyne compound. And/or like.
Synthesis of the C1-C27 Fragment of Stambomycin D Validates Modular Polyketide Synthase-Based Stereochemical Assignments
Anderson, Edward A.,Bernasconi, Alice,Blanco, Araceli,Challis, Gregory L.,Chintalapudi, Venkaiah,Gudmundsson, Haraldur G.,Lim, Jieyan,Song, Lijiang,Tran, Minh
supporting information, p. 7439 - 7444 (2021/10/01)
The stambomycins are a family of bioactive macrolides isolated from Streptomyces ambofaciens. Aside from two stereocenters installed through cytochrome P450 oxidations, their stereochemistry has been predicted by sequence analysis of the polyketide synthase. We report a synthesis of the C1-C27 fragment of stambomycin D, the spectroscopic data of which correlates well with that of the natural product, further validating predictive sequence analysis as a powerful tool for stereochemical assignment of complex polyketide natural products.
Synthesis of chiral branched allylamines through dual photoredox/nickel catalysis
Garbacz, Mateusz,Stecko, Sebastian
supporting information, p. 8578 - 8585 (2021/10/20)
Allylamines are versatile building blocks in the synthesis of various naturally occurring products and pharmaceuticals. In contrast to terminal allylamines, the methods of synthesis of their branched congeners with internal, stereodefined double bonds are less explored. This work describes a new approach for the preparation of allylaminesviacross-coupling of alkyl bromides with simple 3-bromoallylamines by merging the photoredox approach and Ni catalysis. The reaction proceeds under mild conditions, under blue light irradiation, and in the presence of an organic dye, 4CzIPN, as a photocatalyst. The scope of suitable reaction partners is broad, including alkyl bromides bearing reactive functionalities (e.g., esters, nitriles, aldehydes, ketones, epoxides) andN-protected allylamines, as well asN-allylated secondary and tertiary amines and heterocycles. The employment of non-racemic starting materials allows for rapid and easy construction of complex multifunctional allylamine derivatives without the loss of enantiomeric purity.