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  1. Article ; Online: Correction

    Haythem A. Saadeh / Kamal A. Sweidan / Mohammad S. Mubarak

    Molecules, Vol 27, Iss 13, p

    Saadeh et al. Recent Advances in the Synthesis and Biological Activity of 8-Hydroxyquinolines. Molecules 2020, 25 , 4321

    2022  Volume 4306

    Abstract: The author wishes to make the following correction to this paper [.] ...

    Abstract The author wishes to make the following correction to this paper [.]
    Keywords n/a ; Organic chemistry ; QD241-441
    Language English
    Publishing date 2022-07-01T00:00:00Z
    Publisher MDPI AG
    Document type Article ; Online
    Database BASE - Bielefeld Academic Search Engine (life sciences selection)

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  2. Article ; Online: Benzimidazole–Piperazine–Coumarin/Cucurbit[7]uril Supramolecular Photoinduced Electron Transfer Fluorochromes for Detection of Carnosol by Stimuli-Responsive Dye Displacement and pKa Tuning

    Rukayat S. Bojesomo / Khaleel I. Assaf / Haythem A. Saadeh / Lamia A. Siddig / Na’il Saleh

    ACS Omega, Vol 7, Iss 2, Pp 2356-

    2022  Volume 2363

    Keywords Chemistry ; QD1-999
    Language English
    Publishing date 2022-01-01T00:00:00Z
    Publisher American Chemical Society
    Document type Article ; Online
    Database BASE - Bielefeld Academic Search Engine (life sciences selection)

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  3. Article ; Online: Synthesis and biological applications of some novel 8-Hydroxyquinoline urea and thiourea derivatives

    Mohammad A. Khasawneh / Ayesha AlKaabi / Abdelouahid Samadi / Priya Antony / Ranjit Vijayan / Lamya Ahmed Al-Keridis / Haythem A. Saadeh / Nael Abutaha

    Arabian Journal of Chemistry, Vol 15, Iss 7, Pp 103905- (2022)

    2022  

    Abstract: A number of novel urea and thiourea derivatives of 8-hydroxyquinoline have been designed, synthesized and evaluated for their anticancer activities. The structures of the new compounds were established by spectroscopic techniques, 1H NMR, 13C NMR, and ... ...

    Abstract A number of novel urea and thiourea derivatives of 8-hydroxyquinoline have been designed, synthesized and evaluated for their anticancer activities. The structures of the new compounds were established by spectroscopic techniques, 1H NMR, 13C NMR, and mass spectrometry. The in vitro cytotoxicity against MCF7, and MDA-MB-231 cell lines were assessed by MTT assay. Six of the 11 compounds synthesized namely 5b, 5c, 5f, and 6b-d exhibited cytotoxicity with IC50 values ranged between 0.5 and 42.4 µM. Apoptotic features of cells treated with 5b compound were observed via florescent microscopy using DAPI and ethidium bromide/acridine orange staining against MCF-7 cells. Molecular docking of these molecules against 16 potential breast cancer protein revealed that these compounds could interact with the active site of poly (ADP-ribose) polymerase-1 (PARP1), B-cell lymphoma-extra large (Bcl-xL) and PARP5A (Tankyrase 1) by forming hydrogen bonds, π-π interactions and hydrophobic interactions. The docked poses of these molecules were observed to be similar in the active site of each of these targets.
    Keywords 8-Hydroxyquinoline ; Urea ; Thiourea ; Piperazine ; Anticancer ; Apoptosis ; Chemistry ; QD1-999
    Subject code 540
    Language English
    Publishing date 2022-07-01T00:00:00Z
    Publisher Elsevier
    Document type Article ; Online
    Database BASE - Bielefeld Academic Search Engine (life sciences selection)

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  4. Article ; Online: Identification of a Tool Compound to Study the Mechanisms of Functional Selectivity between D2 and D3 Dopamine Receptors

    Irene Reyes-Resina / Abdelouahid Samadi / Gemma Navarro / Haythem A. Saadeh / Mohammad A. Khasawneh / Jordi Mestres / José Marco-Contelles / Rafael Franco

    ACS Omega, Vol 3, Iss 12, Pp 17368-

    2018  Volume 17375

    Keywords Chemistry ; QD1-999
    Language English
    Publishing date 2018-12-01T00:00:00Z
    Publisher American Chemical Society
    Document type Article ; Online
    Database BASE - Bielefeld Academic Search Engine (life sciences selection)

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  5. Article ; Online: New Synthesis and Antiparasitic Activity of Model 5-Aryl-1-methyl-4-nitroimidazoles

    Mustafa M. El-Abadelah / Ibrahim M. Mosleh / Haythem A. Saadeh

    Molecules, Vol 14, Iss 8, Pp 2758-

    2009  Volume 2767

    Abstract: A number of 5-aryl-1-methyl-4-nitroimidazoles 5a-f have been synthesized in good yields by the Suzuki coupling reaction between 5-chloro-1-methyl-4-nitroimidazole (3) and arylboronic acids 4a-f, aided by dichlorobis-(triphenylphosphine)palladium(II), ... ...

    Abstract A number of 5-aryl-1-methyl-4-nitroimidazoles 5a-f have been synthesized in good yields by the Suzuki coupling reaction between 5-chloro-1-methyl-4-nitroimidazole (3) and arylboronic acids 4a-f, aided by dichlorobis-(triphenylphosphine)palladium(II), K2CO3, and tetrabutylammonium bromide in water at 70-80 °C. Compounds 5a-f were characterized by elemental analysis, NMR and MS spectral data. On the basis of in vitro screening data, 5-(3-chlorophenyl)-1-methyl-4-nitro-1H-imidazole (5f)exhibited potent lethal activity against Entamoeba histolytica and Giardia intestinalis with IC50 = 1.47 µM/mL, a value lower by a factor of two than that of the standard drug, metronidazole. The boosted activity of 5f was not accompanied by any increased cytotoxicity.The rest of the series also exhibited potent antiparasitic activity with IC50 valuesin the 1.72-4.43 µM/mL range. The cytotoxicity of the derivatives 5c and 5e was increased compared to the precursor compound, metronidazole, although they remain non-cytotoxic at concentrations much higher than the antiparasitic concentration of the two derivatives.
    Keywords 5-chloro-1-methyl-4-nitroimidazole ; arylboronic acids ; Suzuki coupling ; 5-aryl-1-methyl-4-nitroimidazoles ; antiparasitic activity ; Organic chemistry ; QD241-441
    Subject code 540
    Language English
    Publishing date 2009-07-01T00:00:00Z
    Publisher MDPI AG
    Document type Article ; Online
    Database BASE - Bielefeld Academic Search Engine (life sciences selection)

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  6. Article ; Online: Synthesis of Novel Hybrid Molecules from Precursors With Known Antiparasitic Activity

    Ibrahim M. Mosleh / Haythem A. Saadeh / Mohammad S. Mubarak

    Molecules, Vol 14, Iss 4, Pp 1483-

    2009  Volume 1494

    Abstract: Three novel new compounds derived from antiparasitic precursors have been synthesized and tested for their antiamoebic and antigiardial activities. The condensation of 2-(2-methyl-5-1H-nitroimidazolyl)ethylamine (6) with 5-nitro-2-furylacrylic acid (7) ... ...

    Abstract Three novel new compounds derived from antiparasitic precursors have been synthesized and tested for their antiamoebic and antigiardial activities. The condensation of 2-(2-methyl-5-1H-nitroimidazolyl)ethylamine (6) with 5-nitro-2-furylacrylic acid (7) gave 3-(5-nitrofuran-2-yl)-N-[2-(5-nitroimidazol-1-yl)ethyl]acrylamide (8). Condensation of 7 with 7-chloro-4-(piperazin-1-yl)quinoline (9) afforded 1-[4-(7-chloroquinolin-4-yl)piperazin-1-yl)-3-(5-nitrofuran-2-yl)propenone as a mixture of two isomers; 10-a (the E-isomer) and 10-b (the Z-isomer). In addition, the reaction of 9 with 1-(2-bromoethyl)-2-methyl-5-nitroimidazole (11) in the presence of K2CO3 and NaI yielded 7-chloro-4-(4-[2-(5-nitroimidazol-1-yl)ethyl]-piprazin-1-yl)quinoline (12). On the basis of preliminary screening data for these new compounds, compound 12 exhibited potent lethal activities against Entamoeba histolytica and Giardia intestinalis; its IC50 ( about 1 µM) was lower, at least by a factor of five, compared to the standard drug, metronidazole. In addition, the IC50 of compound 12 against the tested parasites is 600 times below that against Hep-2 and Vero cells. Compounds 8 and 10-a also exhibited potent or moderate antiamoebic and antigiardial activities with IC50 values of about 5.5 µM, and 140 µM, respectively, against the tested parasites. These two hybrid molecules, 8, 10-a, were also non-cytotoxic at the lethal concentrations against the parasites.
    Keywords Hybrid Molecules ; Metronidazole ; Chloroquine ; Entamoeba Histolytica ; Giardia Intestinalis ; Organic chemistry ; QD241-441
    Subject code 540
    Language English
    Publishing date 2009-04-01T00:00:00Z
    Publisher MDPI AG
    Document type Article ; Online
    Database BASE - Bielefeld Academic Search Engine (life sciences selection)

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