scholarly journals Synthesis, Characterization, and Biological Evaluations of 1,3,5-Triazine Derivatives of Metformin Cyclization with Berberine and Magnolol in the Presence of Sodium Methylate

Molecules ◽  
2017 ◽  
Vol 22 (10) ◽  
pp. 1752 ◽  
Author(s):  
Han Cao ◽  
Shili Liao ◽  
Wenjing Zhong ◽  
Xuerong Xiao ◽  
Jiancheng Zhu ◽  
...  
Molecules ◽  
2021 ◽  
Vol 26 (4) ◽  
pp. 1028
Author(s):  
Monnaya Chalermnon ◽  
Sarocha Cherdchom ◽  
Amornpun Sereemaspun ◽  
Rojrit Rojanathanes ◽  
Tanatorn Khotavivattana

Twelve derivatives of biguanide-derived 1,3,5-triazines, a promising class of anticancer agent, were synthesised and evaluated for their anticancer activity against two colorectal cancer cell lines—HCT116 and SW620. 2c and 3c which are the derivatives containing o-hydroxyphenyl substituents exhibited the highest activity with IC50 against both cell lines in the range of 20–27 µM, which is comparable to the IC50 of cisplatin reference. Moreover, the potential use of the calcium citrate nanoparticles (CaCit NPs) as a platform for drug delivery system was studied on a selected 1,3,5-triazine derivative 2a. Condition optimisation revealed that the source of citrate ions and reaction time significantly influence the morphology, size and %drug loading of the particles. With the optimised conditions, “CaCit-2a NPs” were successfully synthesised with the size of 148 ± 23 nm and %drug loading of up to 16.3%. Furthermore, it was found that the release of 2a from the synthesised CaCit-2a NPs is pH-responsive, and 2a could be control released under the acidic cancer environment. The knowledge from this study is perceptive for further development of the 1,3,5-triazine-based anticancer drugs and provide the platform for the incorporation of other drugs in the CaCit NPs in the future.


1975 ◽  
Vol 30 (7-8) ◽  
pp. 603-605 ◽  
Author(s):  
Nazmi Abdel Latif Kassab ◽  
Abdel Hamid Harhash ◽  
Sanna Osman Abd Allah

The 5-arylazo-1-methyl-2-benzyl-2-imidazolin-4-ones (1 a-c) undergo ring cleavage with 1% aqueous sodium hydroxide solution affording α-arylhydrazono-phenacetyl-sarcosine amide (2). Prolonged heating of 1 and 2 with the same reagent yields the cyanamide (3). On the other hand, when 1 a-c were refluxed with acetic acid the triazinones (4) were obtained. The latter adds one mole of Grignards reagent to yield the 5-hydroxy-1,2,4-triazine derivatives (5).


1931 ◽  
Vol 4 (3) ◽  
pp. 264-274 ◽  
Author(s):  
Charles F. H. Allen

In the presence of a small amount of sodium methylate, cyclohexanone and benzil form an addition product, which is a "semicyclic" 1:4-diketone. No derivatives of a bicyclic cyclo-heptane were found. Its most conspicuous chemical property is its sensitivity to mineral acids; among the reaction products is found a diphenyltetrahydrocumarone. Although the addition product exhibits the phenomenon of halochromism, the existence of a perchlorate is doubtful, and it did not form a free radical.


1962 ◽  
Vol 27 (11) ◽  
pp. 4054-4056 ◽  
Author(s):  
John T. Shaw ◽  
Elizabeth R. Nicottra ◽  
Richard K. Madison

2012 ◽  
Vol 9 (2) ◽  
pp. 583-592 ◽  
Author(s):  
Vikas D. Ghule ◽  
S. Radhakrishnan ◽  
Pandurang M. Jadhav ◽  
Surya P. Tewari

s-Triazine is the essential candidate of many energetic compounds due to its high nitrogen content, enthalpy of formation and thermal stability. The present study explores s-triazine derivatives in which different -NO2, -NH2and -N3substituted azoles are attached to the triazine ring via C-N linkage. The density functional theory is used to predict geometries, heats of formation and other energetic properties. Among the designed compounds, -N3derivatives show very high heats of formation. The densities for designed compounds were predicted by using the crystal packing calculations. Introduction of -NO2group improves density as compared to -NH2and -N3, their order of increasing density can be given as NO2>N3>NH2. Analysis of the bond dissociation energies for C-NO2, C-NH2and C-N3bonds indicates that substitutions of the -N3and -NH2group are favorable for enhancing the thermal stability ofs-triazine derivatives. The nitro and azido derivatives of triazine are found to be promising candidates for the synthetic studies.


1984 ◽  
Vol 49 (2) ◽  
pp. 549-554 ◽  
Author(s):  
Jana Barthová ◽  
Marie Tichá ◽  
Peter Gemeiner ◽  
Danica Mislovičová

The interaction of lactate dehydrogenase with high-molecular-weight derivatives of Cibacron Blue was followed by measuring the reaction kinetics and by means of affinity electrophoresis. The dye was covalently bound to dextrans with relative molecular mass ranging from 5 000 to 2 000 000 and to hydroxyethyl-starches with relative molecular mass from 130 000 to 2 000 000. In the case of dextran derivatives of Cibacron Blue, various degrees of substitution by the dye were tested. Measurement of kinetics showed that the Cibacron Blue derivatives competed with NADH for the binding site on the enzyme and that when the dye was bound to a polysaccharide, the affinity of lactate dehydrogenase to the dye decreased. Both methods used confirmed that the strength of interaction did not depend on the relative molecular mass of the polysaccharide carrier or on the degree of substitution. The interaction of lactate dehydrogenase with hydroxyethyl-starch derivatives of Cibacron Blue was weaker than with dextran derivatives.


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