1685-25-2Relevant academic research and scientific papers
COMPOUNDS AND COMPOSITIONS FOR THE TREATMENT OF TUMORS
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Page/Page column 162-163, (2021/06/22)
The present invention relates to compounds of Formula (Ia) or pharmaceutically acceptable salts, hydrates, solvates, clathrates, polymorphs, stereoisomers thereof. It further discloses a pharmaceutical composition comprising compounds of Formula (Ia) and the use of compounds of Formula (Ib), in particular for the use in the treatment of diseases or disorders wherein disrupting Rad51-BRCA2 interaction is beneficial.
One-Pot Synthesis of 4-Quinolone via Iron-Catalyzed Oxidative Coupling of Alcohol and Methyl Arene
Lee, Seok Beom,Jang, Yoonkyung,Ahn, Jiwon,Chun, Simin,Oh, Dong-Chan,Hong, Suckchang
supporting information, p. 8382 - 8386 (2020/11/18)
Herein, we describe the iron(III)-catalyzed oxidative coupling of alcohol/methyl arene with 2-amino phenyl ketone to synthesize 4-quinolone. Alcohols and methyl arenes are oxidized to the aldehyde in the presence of an iron catalyst and di-tert-butyl peroxide, followed by a tandem process, condensation with amine/Mannich-type cyclization/oxidation, to complete the 4-quinolone ring. This method tolerates various kinds of functional groups and provides a direct approach to the synthesis of 4-quinolones from less functionalized substrates.
Dihydroquinazolines as a novel class of Trypanosoma brucei trypanothione reductase inhibitors: Discovery, synthesis, and characterization of their binding mode by protein crystallography
Patterson, Stephen,Alphey, Magnus S.,Jones, Deuan C.,Shanks, Emma J.,Street, Ian P.,Frearson, Julie A.,Wyatt, Paul G.,Gilbert, Ian H.,Fairlamb, Alan H.
supporting information; experimental part, p. 6514 - 6530 (2011/12/02)
Trypanothione reductase (TryR) is a genetically validated drug target in the parasite Trypanosoma brucei, the causative agent of human African trypanosomiasis. Here we report the discovery, synthesis, and development of a novel series of TryR inhibitors based on a 3,4-dihydroquinazoline scaffold. In addition, a high resolution crystal structure of TryR, alone and in complex with substrates and inhibitors from this series, is presented. This represents the first report of a high resolution complex between a noncovalent ligand and this enzyme. Structural studies revealed that upon ligand binding the enzyme undergoes a conformational change to create a new subpocket which is occupied by an aryl group on the ligand. Therefore, the inhibitor, in effect, creates its own small binding pocket within the otherwise large, solvent exposed active site. The TryR-ligand structure was subsequently used to guide the synthesis of inhibitors, including analogues that challenged the induced subpocket. This resulted in the development of inhibitors with improved potency against both TryR and T. brucei parasites in a whole cell assay.
Studies on the synthesis of 5-benzyl-1,3,4-benzotriazepines from 2-isothiocyanatodesoxybenzoine
Morgenstern,Richter,Ahrens
, p. 25 - 28 (2007/10/02)
The reaction of 2-isothiocyanatodesoxybenzoine prepared from 2-aminodesoxybenzoine and thiophosgene in good yield and 2-aminoethanol or methylhydrazine supplied a 4-hydroxy-1,2,3,4-tetrahydroquinazoline and an open chained thiosemicarbazide derivative, respectively. When heating, both compounds react under loss of water. The latter forms the 5-benzyl-3-methyl-2-thioxo-2,3-dihydro-1H-1,3,4-benzotriazepine which can be alkylated at the sulphur atom and transformed into the 2-oxo analog.
