scholarly journals Amino- and polyaminophthalazin-1(2H)-ones: synthesis, coordination properties, and biological activity

2021 ◽  
Vol 17 ◽  
pp. 558-568
Author(s):  
Zbigniew Malinowski ◽  
Emilia Fornal ◽  
Agata Sumara ◽  
Renata Kontek ◽  
Karol Bukowski ◽  
...  
Keyword(s):  
Biological Activity ◽  
Metal Ion ◽  
Spectroscopic Data ◽  
Anticancer Activities ◽  
Biological Screening ◽  
Biological Assays ◽  
Palladium Catalyzed ◽  
Amino Derivatives ◽  
Derivatives Of ◽  
Ht 29

Amino- and polyaminophthalazinones were synthesized by the palladium‐catalyzed amination (alkyl- and arylamines, polyamines) of 4-bromophthalazinones in good yields. The coordinating properties of selected aminophthalazinones towards Cu(II) ions were investigated and the participation of the nitrogen atoms in the complexation of the metal ion was shown. A biological screening of the potential cytotoxicity of selected synthesized compounds on HT-29 and PC-3 cell lines, as well as on the L-929 cell line, proved that some amino derivatives of phthalazinone show interesting anticancer activities. The detailed synthesis, spectroscopic data, and biological assays are reported.

scholarly journals Phenolic Fractions from Vaccinium vitis-idaea L. and Their Antioxidant and Anticancer Activities Assessment

Antioxidants ◽  
2020 ◽  
Vol 9 (12) ◽  
pp. 1261
Author(s):  
Gabriele Vilkickyte ◽  
Lina Raudone ◽  
Vilma Petrikaite
Keyword(s):  
Antioxidant Activity ◽  
Biological Activity ◽  
Cell Lines ◽  
Radical Scavenging ◽  
Colon Adenocarcinoma ◽  
Human Colon ◽  
Anticancer Activities ◽  
Cell Renal Cell Carcinoma ◽  
Human Malignant Melanoma ◽  
Ht 29

Lingonberry leaves and fruits are associated with a range of potential bioactivities related to their phenolic content and composition, but the identification of major biological activity markers remains limited. The present study aimed at the isolation of lingonberry phenolic fractions and biological activity evaluation of them. Crude dry extracts of lingonberry leaves and fruits were fractionated by chromatography using Sephadex LH-20 and analyzed by validated HPLC-PDA method. For each fraction, the anticancer activity against human clear cell renal cell carcinoma (CaKi-1), human colon adenocarcinoma (HT-29), and human malignant melanoma (IGR39) cell lines was determined using MTT assay, and the radical scavenging, reducing, and chelating activities were investigated using ABTS, FRAP, and FIC assays, respectively. Further, 28 phenolics were identified and quantified in the crude extract of lingonberry leaves and 37 in the extract of fruits. These compounds, during fractionation steps, were selectively eluted into active fractions, enriched with different groups of phenolics—monophenols, anthocyanins, phenolic acids, catechins, flavonols, or proanthocyanidins. Fractions of lingonberry leaves and fruits, obtained by the last fractionation step, proved to be the most active against tested cancer cell lines and possessed the greatest antioxidant activity. In this perspective, the predominant compounds of these fractions—polymeric and mainly A-type dimeric proanthocyanidins—also quercetin can be considered to be anticancer and antioxidant activity markers of lingonberries.

Synthesis and Properties of Methyl-, Formyl- and Amino-Diazaphenanthrene

1994 ◽  
Vol 47 (11) ◽  
pp. 2129 ◽  
Author(s):  
L Chrzastek ◽  
B Mianowska ◽  
W Sliwa
Keyword(s):  
Biological Activity ◽  
Activity Data ◽  
Amino Derivatives ◽  
Derivatives Of

Methyl, formyl and amino derivatives of the isomeric benzo [c][1,5] naphthyridine and benzo [f][1,7] naphthyridine have been obtained, and their structures confirmed by 1H n.m.r. spectroscopy. Biological activity data (MIC) for some methyl and formyl derivatives are presented.

Synthesis and biological activity of certain amino-derivatives of 5α-steroids

2006 ◽  
Vol 42 (3) ◽  
pp. 322-324 ◽  
Author(s):  
M. I. Merlani ◽  
L. Sh. Amiranashvili ◽  
K. G. Mulkidzhanyan ◽  
E. P. Kemertelidze
Keyword(s):  
Biological Activity ◽  
Amino Derivatives ◽  
Derivatives Of

scholarly journals FLAVONOID COMPOUNDS FROM ARTEMISIA GLABELLA KAR. ET. KIR., SYNTHESIS ON THEIR BASIS AND BIOLOGICAL ACTIVITY

2018 ◽  
pp. 215-222
Author(s):  
Габиден (Gabiden) Маратович (Maratovich) Байсаров (Baysarov) ◽  
Айдана (Аjdana) Рахманиякызы (Rakhmaniyakyzy) Жуматаева (Zhumatayeva) ◽  
Гулим (Gulim) Кенесбековна (Kenesbekovna) Мукушева (Mukusheva) ◽  
Эльвира (El'vira) Эдуардовна (Eduardovna) Шульц (Shul'ts) ◽  
Роза (Roza) Батталовна (Battalovna) Сейдахметова (Seydakhmetova) ◽  
...  
Keyword(s):  
Biological Activity ◽  
Raw Materials ◽  
Hepatoprotective Activity ◽  
Biologically Active ◽  
Secondary Amines ◽  
Moderate Activity ◽  
Amino Derivatives ◽  
Anti Inflammatory ◽  
Derivatives Of

As a result of complex chemical processing of medicinal raw materials of Artemisia glabella Kar. et Kir., including CO2 extraction and lactones isolation, we have investigated the chemical composition of flavonoids to select the biologically active ones and carry out modifications on their basis. Two flavonoids pectolinaringenin and cirsilineol have been isolated by partition chromatography from the secondary raw materials of Artemisia glabella Kar. et. Kir. and identified. To obtain new biologically active compounds, we have synthesized new amino derivatives of cirsilineol by the Mannich reaction with secondary amines (piperidine and N-methylpiperazine) in isopropanol with the presence of dimethylaminopyridine. In proton NMR spectrum of the synthesized compounds there are proton signals of the initial cirsilineol fragment; however, there is no N-8 proton signal, besides other signals typical for amines’ benzene ring have been observed at 1.53–3.90 ppm. It means that reaction occurred at the C-8 position of carbon in ring A. The synthesized compounds have been studied for various types of biological activity typical for this class, including hepatoprotective and anti-inflammatory activities. Amino derivatives of cirsilineol exhibit a moderate activity against HepG2 cell line, while cirsilineol at a dose of 5 mg/ml expresses a pronounced hepatoprotective activity. Moreover, all samples at a dose of 25 mg/kg show poor anti-inflammatory effects on the model of acute exudative reaction in vivo.

Synthesis and Biological Activity of 3- and 5-Amino Derivatives of Pyridine-2-carboxaldehyde Thiosemicarbazone

1996 ◽  
Vol 39 (13) ◽  
pp. 2586-2593 ◽  
Author(s):  
Mao-Chin Liu ◽  
Tai-Shun Lin ◽  
Joseph G. Cory ◽  
Ann H. Cory ◽  
Alan C. Sartorelli
Keyword(s):  
Biological Activity ◽  
Amino Derivatives ◽  
Derivatives Of

scholarly journals Synthesis and antifungal properties of papulacandin derivatives

2012 ◽  
Vol 8 ◽  
pp. 732-737 ◽  
Author(s):  
Marjolein van der Kaaden ◽  
Eefjan Breukink ◽  
Roland J Pieters
Keyword(s):  
Biological Activity ◽  
Coupling Reaction ◽  
Cross Coupling ◽  
Side Chain ◽  
Aryl Iodide ◽  
Glucan Synthase ◽  
Cross Coupling Reaction ◽  
Acyl Side Chain ◽  
Palladium Catalyzed ◽  
Derivatives Of

Derivatives of an antifungal agent that targets the β-(1,3)-D-glucan synthase, papulacandin D, were synthesized and tested for activity. The papulacandin D structure contains a challenging benzannulated spiroketal unit, which is introduced in a palladium-catalyzed cross-coupling reaction of a glycal silanolate and an aryl iodide followed by an oxidative spiroketalization. Four different variants were made, differing in the nature of the acyl side chain with respect to the length, and in the number and stereochemistry of the double bonds. Moderate biological activity was observed for the derivatives with a side chain based on palmitic acid and linoleic acid.

Synthesis and biological activity of nucleoside analogs involving modifications in the carbohydrate ring

1985 ◽  
Vol 63 (8) ◽  
pp. 2149-2161 ◽  
Author(s):  
Walter A. Szarek ◽  
B. Mario Pinto ◽  
Masaharu Iwakawa
Keyword(s):  
Biological Activity ◽  
Cell Growth ◽  
Antitumor Activity ◽  
Nucleoside Analogs ◽  
Hela Cell Line ◽  
Biological Screening ◽  
Naturally Occurring ◽  
Derivatives Of ◽  
Substituted 1

The synthesis of a variety of nucleoside analogs involving modifications in the carbohydrate ring is described. In particular, 6-substituted purin-9-yl derivatives of 1-oxa-4-thiacyclohexane and 1,4-dioxacyclohexane have been synthesized. A number of 6-chloropurin-9-yl derivatives of substituted 1-oxa-4-thiacyclohexane have also been derived from the parent compounds by way of a Pummerer rearrangement. A route to nucleoside analogs of 1-oxa-4-thiacyclohexane from naturally occurring nucleosides is illustrated for the case of inosine. A route to nucleoside analogs in which the carbohydrate moiety is replaced by an acyclic moiety bearing α,β-unsaturated esters is also illustrated for the case of uridine. The results of biological screening of these analogs and others previously synthesized in our program against leukemia L-1210 cells in vitro are presented; some of these compounds showed marginal antitumor activity. The screening results of selected compounds against the human HeLa cell line in vitro are also presented; none of the compounds that were tested showed significant inhibitory activity of cell growth.

scholarly journals Antibiotics Aminosidin. II. Some Amino Derivatives of Aminosidin and Their Biological Activity

1973 ◽  
Vol 21 (3) ◽  
pp. 609-615 ◽  
Author(s):  
HYOZO TANIYAMA ◽  
YOSUKE SAWADA ◽  
SHIGEO TANAKA
Keyword(s):  
Biological Activity ◽  
Amino Derivatives ◽  
Derivatives Of

Synthesis and preliminary studies of biological activity of amino derivatives of 4-azatricyclo- [5.2.1.02,6]dec-8-ene-3,5-dione with silicon in the structure

2015 ◽  
Vol 21 (1) ◽  
Author(s):  
Mariola Napiórkowska ◽  
Marcin Cieślak ◽  
Julia Kaźmierczak-Barańska ◽  
Karolina Królewska ◽  
Aleksandra Czapla ◽  
...  
Keyword(s):  
Biological Activity ◽  
Amino Derivatives ◽  
Cyclic Imides ◽  
Derivatives Of

AbstractA series of 38 new derivatives of cyclic imides containing silicon in the structure was synthesized and characterized by

scholarly journals Synthesis, Acaricidal, Bacteriostatic Activity Among the Amino Derivatives 5,7-Dichloro-4,6-Dinitrobenzofuroxana

2019 ◽  
Vol 8 (2) ◽  
pp. 11-15
Author(s):  
L. V. Spatlova
Keyword(s):  
Biological Activity ◽  
Amino Derivative ◽  
Bacteriostatic Activity ◽  
Hazard Class ◽  
Reaction Conditions ◽  
Low Concentrations ◽  
Wide Range ◽  
Amino Derivatives ◽  
New Compounds ◽  
Derivatives Of

Introduction. In recent years, interest in the compounds of the benzofuroxane series has increased, because they have a wide range of biological activity, and in addition are donors of nitric oxide. In the scientific literature, many works are related to the synthesis and study of the biological activity of 5-nitro-4,6-dichlorobenzofuroxane amino derivatives, whereas amino derivatives of the 5,7-dichlor-4,6-dinitrobenzofuroxane substrate have been poorly studied.Aim. Is the synthesis of new amino derivatives of 5,7-dichloro-4,6-dinitrobenzofuroxane and the study of their biological activity.Materials and methods. Investigated the reaction of condensation of 5,7-dichloro-4,6-dinitrobenzofuroxane with different aromatic amines, containing functional groups of acceptor character in their structure were selected. In order to increase the yield for each specific reaction, the reaction conditions were selected (the reaction temperature, medium, and the amount of amine). The structure of the compounds confirmed IR, NMR spectra and elemental analysis.Results and discussion. New compounds in the 5,7-diamino-4,6-dinitrobenzofuroxane series were obtained. Acute toxicity, acaricidal and bacteriostatic activity against Escherichia coli and Staphylococcus aureus were studied. The obtained compounds were found to have high pharmacological activity, superior to the comparison drug (Chlorophos and Creolin).Conclusion. Most of the amino derivative synthesized 5,7-dichloro-4,6-dinitrobenzofuroxane have a high activity against mites and bacteria. Compounds containing in their structure chlorine and methyl radicals, have biological activity at low concentrations, are low-toxic and belong to the 4th hazard class.

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