scholarly journals Synthesis and study of the anticancer activity of some new 7H-[1,2,4]triazolo [3,4-b][1,3,4]thiadiazines

2021 ◽  
Vol 14 (3) ◽  
pp. 320-327
Author(s):  
I. I. Myrko ◽  
T. I. Chaban ◽  
V. V. Ohurtsov ◽  
I. V. Drapak ◽  
V. S. Matiichuk
Keyword(s):  
Nmr Spectroscopy ◽  
Anticancer Activity ◽  
1H Nmr ◽  
Elemental Analysis ◽  
Anticancer Agents ◽  
1H Nmr Spectroscopy ◽  
Analysis Data ◽  
Elemental Analysis Data ◽  
Tumor Cell Death ◽  
Secondary Stage

The problem of finding effective low-toxic anticancer agents is one of the most important in modern medicine and pharmacy. Despite a large selection of anticancer drugs and a variety of mechanisms of their action, the effectiveness of existing drugs continues to be insufficient. Among the numerous natural and synthetic heterocyclic compounds that exhibit anticancer activity, 7H-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazine derivatives, which are able to initiate different pathways of tumor cell death. Based on this, the synthesis of new derivatives of this class of compounds and the study of their anticancer properties is relevant. The aim of the work is to synthesis of new 7H-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazines and study their anticancer activity. Materials and methods. It was used methods of organic synthesis, physical and chemical methods of analysis organic compounds (1H NMR spectroscopy, elemental analysis). Results. In order to obtain new 7H-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazines, the interaction implemented of 4-amino-4H-[1,2,4]triazole-3-thiols with the corresponding bromoacetophenones. The reaction proceeds by heating the above reagents in alcohol with the closure of the thiadiazine ring and the formation of 7H-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazine systems. The structure of all synthesized compounds was confirmed by 1H NMR spectroscopy and elemental analysis data. The study of the anticancer activity of the synthesized compounds was carried out in the framework of the international scientific program DTP (Developmental Therapeutics Program) of the National Cancer Institute (NCI, Bethesda, Maryland, USA). It was found that the synthesized compounds exhibited different levels of anticancer activity. The most active among the tested substances was compound 3j with an average GP value of 28.73. The most sensitive to it were the lines of melanoma MDA-MB-435 and SK-MEL-2, kidney cancer A498 and RXF 393, CNS cancer SNB-75, and non-small cell lung cancer NCI-H522. The secondary stage of studies of this compound confirmed its high anticancer activity against most cancer cell lines. Conclusions. As a result of the interaction of 4-amino-4H-[1,2,4]triazole-3-thiols with the relevant bromoacetophenones, a series of new triazolo[3,4-b][1,3,4]thiadiazines was not described in the literature was synthesized. Testing the synthesized compounds for the antitumor activity made it possible to isolate 1 highly active compound with a pronounced anticancer effect, which in terms of activity approaches or exceeds the known drugs 5-fluorouracil (5-FU) and cisplatin, as well as an anticancer agent, curcumin.  

scholarly journals Synthesis some 4-substituted 9,10-anthraquinones

2020 ◽  
Vol 8 (1) ◽  
pp. 58-65
Author(s):  
Vasyl Shupeniuk ◽  
Tetyana Taras ◽  
Oksana Sabadakh ◽  
Eugene Luchkevich ◽  
Yurii Kornii
Keyword(s):  
Nmr Spectroscopy ◽  
1H Nmr ◽  
Elemental Analysis ◽  
13C Nmr ◽  
Coupling Reaction ◽  
13C Nmr Spectroscopy ◽  
Analysis Data ◽  
Elemental Analysis Data ◽  
Ullmann Coupling

New 4-substituted 9,10-anthraquinones (6 compouds) with amino derivations fragments were synthesized through the substitution of the bromaminic acid by amines using the Ullmann coupling reaction. The structures of the synthesized compounds were determined using LC-MS, 1H NMR, 13C NMR spectroscopy, and elemental analysis data.

scholarly journals The synthesis and characterization of some new diazoamino derivatives

2010 ◽  
Vol 16 (1) ◽  
pp. 89-95
Author(s):  
Mihaela Mocanu
Keyword(s):  
1H Nmr ◽  
Bioactive Compounds ◽  
Elemental Analysis ◽  
Analysis Data ◽  
Biological Properties ◽  
Synthesis And Characterization ◽  
Elemental Analysis Data ◽  
Spectral Measurements ◽  
Inflammatory Processes

The sulfonamidic moiety is much encountered in structures of bioactive compounds. In the present paper the studies on the sulfonamidated aryloxyalkylcarboxylic acids are extended by their attaching on certain substrata able to confer some special biological properties to the final products, such as anti-tumor and antioxidant actions useful in treating inflammatory processes, ulcer, convulsions and diabetes, as well as a herbicidal action. The stepwise syntheses of the sulfonamidated aryloxyalkylcarboxylic acid derivatives and their characterization by elemental analysis data and IR, 1H-NMR and UV-Vis spectral measurements are described. The newly obtained compounds could show potential pharmaceutical and herbicide properties.

SYNTHESIS AND PROPERTIES OF INTERACTION PRODUCTS OF TRIS[TRI(BUTOXY)TITANATE]BORON AND ALIPHATIC FLUORINATED ALCOHOLS

2018 ◽  
Vol 59 (1) ◽  
pp. 75 ◽  
Author(s):  
N.Ya. Kuzmenko ◽  
S.N. Kuzmenko ◽  
O.V. Skrinnik ◽  
V.V. Bugrym
Keyword(s):  
Nmr Spectroscopy ◽  
Molecular Mass ◽  
1H Nmr ◽  
Elemental Analysis ◽  
1H Nmr Spectroscopy ◽  
Alkoxy Group ◽  
Partial Substitution ◽  
Fluorinated Alcohols ◽  
Analysis Determination

Synthesis and properties of products based on tris[[tri(butoxy)titanate]boron with complete or partial substitution of butoxy groups linked with titanium by fluorinated alkoxy group were described. Extracted products were liquid or solid substances which are high soluble in aliphatic-, aromatic- chloraromatic- and chlorinated hydrocarbons, low alcohols, and ketone. Their structure was confirmed by elemental analysis, determination of molecular mass, IR and 1H NMR spectroscopy.

scholarly journals Tetracyclic Heteroaromatic Systems-Synthesis of Ethoxycarbonylphenylpyrido[3',2':5,6] Thiopyranoquinolines

2021 ◽  
Vol 64 (3) ◽  
pp. 191-194
Author(s):  
Muhammad Naeem Khan ◽  
Misbahul Ain Khan ◽  
Noreen Aslam ◽  
Pir Bakhsh Khan ◽  
Ehsan ul Haq
Keyword(s):  
1H Nmr ◽  
Elemental Analysis ◽  
Mass Spectra ◽  
Ethyl Pyruvate ◽  
Analysis Data ◽  
Elemental Analysis Data

7-benzylideneamino-5H-thiochromeno[2,3-b]pyridin-5-ones and 9-benzylideneamino-5H-thio- chromeno[2,3-b]pyridin-5-ones, on reaction with ethyl pyruvate to afford 1-ethoxycarbonyl-3-phenyl-12H- pyrido[3',2':5,6]thiopyrano[3,2-f]quinoline-12-ones and 4-ethoxycarbonyl-2-phenyl-7H- pyrido[3',2':5,6]thiopyrano[3,2-h]quinoline-7-ones respectively by the two different methods. These products were precipitated by addition of ethanol, water (1:1), were purified by recrystalizing from appropriate solvents and were characterized from their IR, 1H-NMR, mass spectra and elemental analysis data.  

SYNTHESIS AND EVALUATION OF SOME NEWER QUINAZOLINONYL SUBSTITUTED BENZOXAZEPINYL / BENZOTHIAZEPINYL INDOLES AS POTENT ANTICONVULSANT AGENTS

INDIAN DRUGS ◽  
2019 ◽  
Vol 56 (03) ◽  
pp. 18-24
Author(s):  
Archana ◽  
Keyword(s):  
Nmr Spectroscopy ◽  
Acute Toxicity ◽  
1H Nmr ◽  
Elemental Analysis ◽  
Anticonvulsant Activity ◽  
1H Nmr Spectroscopy ◽  
Standard Drug ◽  
Anticonvulsant Agents ◽  
Phenytoin Sodium

new series of 3-[3-amino-2-methyl-6-substituted quinazolin-4(3H)-onyl chalconyl)-2-substituted indoles (3-8), 3-[3-Amino-2-methyl-6- substituted quinazolin-4(3H) -onyl-benzoxazepin/benzo -thiazepin- 2-yl] -2-substituted indoles (9-20) and 3-[3-amino-2-methyl-6-substituted quinazolin-4(3H) -onyl-3- (sub-stituted phenylaminomethylene) -benzoxazepin/benzothizepin-2-yl] -2-substitutedindoles (21-44) were synthesised and evaluated for anticonvulsant activity. All these compounds were screened in vivo, for their anticonvulsant activity and acute toxicity. Coumpund 44 , 3-[3-amino-2-methyl-6-bromoquinazolin- 4(3H)-onyl-3- (chlorophenylaminomethylene)-benzothiazepine-2-yl]-2-chloroindole, was found to be most potent compound of this series , more potent than standard drug phenytoin sodium. The homogeneity of all the compounds have been established by elemental analysis, IR and 1H-NMR spectroscopy.

scholarly journals 4,4′-Di-tert-butyl-2,2′-bipyridinium Trifluoromethanesulfonate

Molbank ◽  
10.3390/m1261 ◽  
2021 ◽  
Vol 2021 (3) ◽  
pp. M1261
Author(s):  
Shintaro Kodama ◽  
Kazuki Bunno ◽  
Akihiro Nomoto ◽  
Akiya Ogawa
Keyword(s):  
Nmr Spectroscopy ◽  
1H Nmr ◽  
Diethyl Ether ◽  
Elemental Analysis ◽  
1H Nmr Spectroscopy ◽  
Trifluoromethanesulfonic Acid ◽  
Simple Method ◽  
Tert Butyl ◽  
Ft Ir ◽  
Direct Use

4,4′-di-tert-butyl-2,2′-bipyridinium trifluoromethanesulfonate was synthesized by stirring 4,4′-di-tert-butyl-2,2′-bipyridine with scandium(III) trifluoromethanesulfonate in acetonitrile, followed by precipitation with diethyl ether. The structure of the new compound was characterized by FT-IR, 1H, 13C{1H} and 19F{1H} NMR spectroscopy and CHN elemental analysis. This is a safe and simple method to obtain mono-protonated bipyridinium trifluoromethanesulfonate without the direct use of trifluoromethanesulfonic acid.

scholarly journals Bimetallic Cd(II) and Hg(II) complexes of 1, 4-bis-(5-H/methyl/chloro-1H-benzimidazol- 2-yl)-1, 2, 3, 4-butanetetraols

2005 ◽  
Vol 70 (8-9) ◽  
pp. 1067-1073 ◽  
Author(s):  
Aydin Tavman
Keyword(s):  
Nmr Spectroscopy ◽  
1H Nmr ◽  
Elemental Analysis ◽  
Metal Ion ◽  
1H Nmr Spectroscopy ◽  
Imidazole Ring ◽  
Molar Conductivity ◽  
Hydroxyl Groups ◽  
Hydroxyl Oxygen ◽  
Oxygen Atoms

The bimetallic complexes of 1,4-bis-(5-H/methyl/chloro-1H-benzimidazol 2-yl)-1,2,3,4-butanetetraols (L1?L3) with CdCl2 and HgCl2 were synthesized and characterized by elemental analysis, molar conductivity, as well as IR and 1H-NMR spectroscopy. The ligands coordinate to the metal ion through all of the hydroxyl oxygen atoms as tetradentate in the Hg(II) complexes of L1?L3 and in the Cd(II) complexes of L2 and L3. In theCd2(L1)Cl4 complex, the ligand acts as tetradentate through the benzimidazole nitrogen atoms and the two oxygen atoms of the hydroxyl groups near the imidazole ring.

scholarly journals New ferrocense containing tiophene derivatives

2019 ◽  
Vol 487 (6) ◽  
pp. 626-629
Author(s):  
E. N. Rodlovskaya ◽  
V. A. Vasnev
Keyword(s):  
Nmr Spectroscopy ◽  
Magnetic Materials ◽  
Schiff Bases ◽  
1H Nmr ◽  
Elemental Analysis ◽  
1H Nmr Spectroscopy

A new 2-amino-4-ferrocenyl-thiophene-3-carbonitrile was synthesized by the Gevald reaction and Schiff bases, precursors for new optoelectronic and magnetic materials, were obtained on its basis. The structures of the synthesized compounds were determined by elemental analysis, IR and 1H NMR spectroscopy.

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