- 1,3-Dipolar cycloreversion of a 1,3,4-oxadiazolidine as a controlled azomethine imine surrogate for pyrazolidine synthesis
-
Azomethine imines were generated in a controlled manner through a thermally allowed 1,3-dipolar cycloreversion of 1,3,4-oxadiazolidines and subsequently trapped with dipolarophiles. This method results in the construction of the pyrazolidine heterocycles. A new method for the selective formation of the key semicarbazide substrate, from benzylidene hydrazone, is also disclosed.
- Khau, Vien V.,Martinelli, Michael J.
-
-
Read Online
- 2-(4-phenyl -1H-1, 2, 3- triazol -1-based) acetic acid and acetylhydrazine compound (by machine translation)
-
The invention belongs to the technical field of medicines, and particularly relates to 2 - (4 - phenyl - 111111111,triazole - 1 1-yl) acetic acid and acetyl hydrazine compound, and a preparation method and application 2 - (4 - thereof, as shown I, II) in: a general formula shown in the specification . . Shows a good result, in an in-vitro kinase experiment, shows good antitumor activity, provides a new idea, for drug design, and provides a new idea for the drug design to provide a new idea for drug design and provides a preparation, method of 2 - (4 - phenyl - 111111111.3-triazole - 1 1-yl) acetic acid and acetylhydrazine new compound, shown in the formula II in an industrialized production. (by machine translation)
- -
-
Paragraph 0063-0065
(2020/05/05)
-
- Synthesis, characterization and anti-cancer activity of hydrazide derivatives incorporating a quinoline moiety
-
Identification of the novel (E)-N1-((2-chloro-7-methoxyquinolin-3-yl)methylene)-3-(phenylthio) propanehydrazide scaffold 18 has led to the development of a new series of biologically active hydrazide compounds. The parent compound 18 and new quinoline derivatives 19-26 were prepared from the corresponding quinoline hydrazones and substituted carboxylic acids using EDC-mediated peptide coupling reactions. Further modification of the parent compound 18 was achieved by replacement of the quinoline moiety with other aromatic systems. All the newly synthesized compounds were evaluated for their anti-cancer activity against the SH-SY5Y and Kelly neuroblastoma cell lines, as well as the MDA-MB-231 and MCF-7 breast adenocarcinoma cell lines. Analogues 19 and 22 significantly reduced the cell viability of neuroblastoma cancer cells with micromolar potency and significant selectivity over normal cells. The quinoline hydrazide 22 also induced G1 cell cycle arrest, as well as upregulation of the p27kip1 cell cycle regulating protein.
- Bingul, Murat,Tan, Owen,Gardner, Christopher R.,Sutton, Selina K.,Arndt, Greg M.,Marshall, Glenn M.,Cheung, Belamy B.,Kumar, Naresh,Black, David StC.
-
-
- AZAPEPTIDES AS CD36 BINDING COMPOUNDS
-
An azapeptide derivative of growth hormone releasing peptide (GHRP) of Formula I: A-(Xaa)a-N(RA)—N(RB)—C(O)-(Xaa′)b-B which binds to CD 36.
- -
-
-
- Diverse alkanones by catalytic carbon insertion into the formyl C-H bond. Concise access to the natural precursor of achyrofuran
-
Over a century ago, the first reactions of diazomethane with aldehydes delivered methyl ketones. In the interim, aldehydes have been homologated with trimethylsilyldiazomethane, diazoacetates, and aryldiazomethanes, on rare occasion with catalysis. This work describes a mild procedure for convergent ketone assembly from nonstabilized diazoalkanes, including examples of chiral ketone synthesis with disubstituted (internal) nucleophiles. The method's remarkable tolerance to steric crowding is showcased in a simple approach to achyrofuran, a complex dibenzofuran.
- Wommack, Andrew J.,Moebius, David C.,Travis, Austin L.,Kingsbury, Jason S.
-
supporting information; experimental part
p. 3202 - 3205
(2009/11/30)
-
- A novel transformation of oximes into hydrazones by hydrazine hydrate
-
We report a novel transformation of different substituted aryl, diaryl, and aralkyloximes into the respective hydrazones using hydrazine hydrate in ethanol at reflux in excellent yields.
- Pasha,Nanjundaswamy
-
p. 3827 - 3831
(2007/10/03)
-
- A convenient preparation of 2-(2-arylidene)- and 2-(2-polyhydroxyalkylidene)hydrazono-4-imidazolidinones with various heterocyclic side chain substituents at position 5 as potential antiviral and antitumor agents
-
A variety of novel 5-[(Z)-arylidene]-2-[(2-(E)-arylidene)hydrazono]4-imidazolidinones 1a-c to 4a,b and 5-[(Z)-arylidene]-2-[(2-(E)-polyhydroxyalkylidene)hydrazono]-4- imidazolidinones 5a-c to 7a-c were prepared from the reaction of 5-[(Z)-arylidene]-2-methylmercaptohydantoins 8a-c with 2-(E)-arylidene hydrazones 13a-d and/or 2-(E)-monosaccharides hydrazones 16a-c. The linear structure, and not that of the angular isomer, has been selected for the products. This structure has been confirmed from a model study of the condensation of 5-[(Z)-2-thienylidene]-2-hydrazono-4-imidazolidinone 9a with benzaldehyde and D-galactose, respectively. The acetylation and benzoylation reactions of compounds 1-7 have been studied. All the new compounds were tested for their potential antiviral and antitumor activities.
- Khodair, Ahmed I.
-
p. 1157 - 1173
(2007/10/03)
-