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    Wyświetlanie 1-4 z 4
    Tytuł:
    Synthesis of kaempferide Mannich base derivatives and their antiproliferative activity on three human cancer cell lines
    Autorzy:
    Nguyen, Van-Son
    Shi, Ling
    Luan, Fang-Qian
    Wang, Qiu-An
    Powiązania:
    https://bibliotekanauki.pl/articles/1039003.pdf
    Data publikacji:
    2015
    Wydawca:
    Polskie Towarzystwo Biochemiczne
    Tematy:
    kaempferide
    flavonoids
    Mannich base derivatives
    synthesis
    antiproliferative activity
    Opis:
    Kaempferide (3,5,7-trihydroxy-4'-methoxyflavone, 1), a naturally occurring flavonoid with potent anticancer activity in a number of human tumour cell lines, was first semisynthesized from naringin. Based on Mannich reaction of kaempferide with various secondary amines and formaldehyde, nine novel kaempferide Mannich base derivatives 2-10 were synthesized. The aminomethylation occurred preferentially in the position at C-6 and C-8 of the A-ring of kaempferide. All the synthetic compounds were tested for antiproliferative activity against three human cancer cell lines (Hela, HCC1954, SK-OV-3) by the standard MTT method. The results showed that compounds 1, 2 and 5-10 were more potent against Hela cells with IC50 values of 12.47-28.24 μM than the positive control cis-platin (IC50 41.25 μM), compounds 5, 6, 8 and 10 were more potent against HCC1954 cells with IC50 values of 8.82-14.97 μM than the positive control cis-platin (IC50 29.68 μM), and compounds 2, 3, 5, 6 and 10 were more potent against SK-OV-3 cells with IC50 values of 7.67-18.50 μM than the positive control cis-platin (IC50 21.27 μM).
    Źródło:
    Acta Biochimica Polonica; 2015, 62, 3; 547-552
    0001-527X
    Pojawia się w:
    Acta Biochimica Polonica
    Dostawca treści:
    Biblioteka Nauki
    Artykuł
    Tytuł:
    Design, Efficient Synthesis, Mechanism of Reaction and Antiproliferative Activity Against Cancer And Normal Cell Lines of A Novel Class of Fused Pyrimidine Derivatives
    Autorzy:
    roaiah, hanaa F.
    Rashdan, Huda R.
    soliman, abdelmohsen
    Muhammed, Zeinab
    Wietrzyk, Joanna
    Milczarek, Magdalena
    Powiązania:
    https://bibliotekanauki.pl/articles/895705.pdf
    Data publikacji:
    2018-06-30
    Wydawca:
    Polskie Towarzystwo Farmaceutyczne
    Tematy:
    anticancer activity
    antiproliferative activity
    Coumarin
    Fused pyrimidines
    3-triazole
    Opis:
    This work concentrated on the utility of hydrazonoyl halides in synthesis of bioactive heterocycles like triazoles, pyrazoles, pyrimidines and their fused derivatives which have a wide spectrum of pharmaceutical value. Herein we discussed the synthesis of new heterocyclic compounds containing fused pyrimidine rings derived from hydrazonoyl halides and their significant pharmaceutical importance as anticancer agents. New fused pyrimidine derivatives bearing 1,2,3-triazole moiety were prepared via reaction of enaminone 2 with and 6-amino-2-thioxo-pyrimidin-4-one and then with hydrazonoyl chlorides 6a-h. In addition 3-amino-6-(2-oxo-2H-chromen-3-yl)pyridine-2-carbonitrile (12) was submitted to react with carbon dioxide to afford 3-(1,2,3,4-tetrahydro-2,4-dithioxopyrido[2,3-d]pyrimidin-7-yl)-2H-chromen-2-one (15), which act as key molecule for synthesis of new series of fused prymidinethione derivatives containing coumarine moiety via its reaction with different selected derivatives of hydrazonoyl halides 6a-h. Structures of the newly synthesized compounds were confirmed using spectral data (IR, H1NMR and Mass spectrometry) and microanalytical methods. Also, they screened for their anticancer activity.
    Źródło:
    Acta Poloniae Pharmaceutica - Drug Research; 2018, 75, 3
    0001-6837
    2353-5288
    Pojawia się w:
    Acta Poloniae Pharmaceutica - Drug Research
    Dostawca treści:
    Biblioteka Nauki
    Artykuł
    Tytuł:
    Otrzymywanie i właściwości biologiczne racemicznych i optycznie czynnych laktonów z pierścieniem aromatycznym w pozycji β
    Synthesis and biological properties of racemic and optically active lactones with aromatic ring on β-position
    Autorzy:
    Gładkowski, Witold
    Powiązania:
    https://bibliotekanauki.pl/articles/27310041.pdf
    Data publikacji:
    2023
    Wydawca:
    Polskie Towarzystwo Chemiczne
    Tematy:
    laktony
    synteza chemoenzymatyczna
    konfiguracja absolutna
    aktywność antyproliferacyjna
    aktywność antyfidantna
    lactones
    chemoenzymatic synthesis
    absolute configuration
    antiproliferative activity
    antifeedant activity
    Opis:
    Natural and synthetic lactones containing an aromatic ring exhibit a number of biological properties, e.g. antiproliferative, antifeedant or antimicrobial activity. This review deals with the synthesis and biological properties of lactones containing an aromatic substituent in the β-position of the lactone ring. The described group of compounds includes halolactones, hydroxylactones, unsaturated lactones and products of reductive dehalogenation of iodolactones. In addition to chemical transformations, biotechnological methods for obtaining optically active lactones have also been described, including the use of lipases in the chemoenzymatic pathway leading to the production of halolactones, kinetic separation of hydroxylactones in the process of enzymatic transesterification, microbial hydrolytic dehalogenation of iodolactones and enantioselective hydrolysis of the lactone ring. The biological activity of the obtained β-aryllactones was also briefly characterized.
    Źródło:
    Wiadomości Chemiczne; 2023, 77, 5-6; 509--531
    0043-5104
    2300-0295
    Pojawia się w:
    Wiadomości Chemiczne
    Dostawca treści:
    Biblioteka Nauki
    Artykuł
    Tytuł:
    Antimicrobial property and antiproliferative activity of Centaurea babylonica (L.) L. on human carcinomas and cervical cancer cell lines
    Autorzy:
    Guvensen, N.C.
    Keskin, D.
    Gunes, H.
    Oktay, M.K.
    Yildirim, H.
    Powiązania:
    https://bibliotekanauki.pl/articles/2083066.pdf
    Data publikacji:
    2019
    Wydawca:
    Instytut Medycyny Wsi
    Tematy:
    Centaura babylonica
    antimicrobial activity
    antiproliferative activity
    A-549
    PC-3
    MCF-7 and HeLa cell lines
    chemical
    composition
    GC-MS
    Opis:
    Introduction and objective. Since antiquity, C. babylonica (L.) L. extracts has been used as a remedy for primary health care in traditional medicine. In this study, a total of seven different crude extracts (acetone, chloroform, hexane, ethylacetate, methanol, ethanol and water) from branches and leaves of C. babylonica (L.) L. were prepared to determine antimicrobial and antiproliferative activity against cancer cell lines. Materials and method. MIC assay was used for antimicrobial activity against gram positive and gram negative bacteria, and one yeast. MTT assay was applied to screen the antiproliferative activity of seven extracts, and to determine dose- and time-dependent effects of the aceton extract on A549, PC-3, MCF-7, and HeLa cell lines. Results. The aceton extract of C.babylonica (L.) L. showed the best antibacterial activity against Bacillus cereus, P. aeruginosa and C. albicans (MIC: 1.6 mg/mL). GC-MS analyses allowed six compounds to be determined; the main constituents of acetone extract from C. babylonica (L.) L. were diacetone alcohol (53.47 %), 1-dexadecene (10.19 %) and 1-tetradecene (8.67 %). In addition, seven different solvent extracts at 500 μg/mL caused antiproliferative activity between 84% – 88%, compared to control. Dose-dependent effects of the extracts on A549 cells indicated that chloroform, ethyl acetate, and aceton extract were the most effective extracts with the IC50 values of 9, 33, and 36 μg/mL, respectively. Conclusions. The results clearly demonstrate that C. babylonica (L.) L. exhibited a strong antimicrobial effect and antiproliferative activity against cancer cells in vitro. Further studies are required to isolate and characterize the active pure compounds responsible for the antimicrobial and antiproliferative activities.
    Źródło:
    Annals of Agricultural and Environmental Medicine; 2019, 26, 2; 290-297
    1232-1966
    Pojawia się w:
    Annals of Agricultural and Environmental Medicine
    Dostawca treści:
    Biblioteka Nauki
    Artykuł
      Wyświetlanie 1-4 z 4

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