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  1. Article ; Online: Phototoxicity of Tridentate Ru(II) Polypyridyl Complex with Expanded Bite Angles toward Mammalian Cells and Multicellular Tumor Spheroids.

    Curley, Rhianne C / Burke, Christopher S / Gkika, Karmel S / Noorani, Sara / Walsh, Naomi / Keyes, Tia E

    Inorganic chemistry

    2023  Volume 62, Issue 32, Page(s) 13089–13102

    Abstract: Tridentate ligand-coordinated ruthenium (II) polypyridyl complexes with large N-Ru-N bite angles have been shown to promote ligand field splitting and reduce singlet-triplet state mixing leading to dramatically extended emission quantum yields and ... ...

    Abstract Tridentate ligand-coordinated ruthenium (II) polypyridyl complexes with large N-Ru-N bite angles have been shown to promote ligand field splitting and reduce singlet-triplet state mixing leading to dramatically extended emission quantum yields and lifetimes under ambient conditions. These effects are anticipated to enhance their photoinduced singlet oxygen production, promoting prospects for such complexes as type II phototherapeutics. In this contribution, we examined this putative effect for [Ru(bqp)(bqpCOOEt)]
    MeSH term(s) Animals ; Cricetinae ; Humans ; CHO Cells ; Coordination Complexes/chemistry ; Coordination Complexes/pharmacology ; Cricetulus ; Ligands ; Neoplasms ; Photochemotherapy ; Photosensitizing Agents/chemistry ; Photosensitizing Agents/pharmacology ; Ruthenium/chemistry ; Ruthenium/pharmacology
    Chemical Substances Coordination Complexes ; Ligands ; Photosensitizing Agents ; Ruthenium (7UI0TKC3U5)
    Language English
    Publishing date 2023-08-03
    Publishing country United States
    Document type Journal Article
    ZDB-ID 1484438-2
    ISSN 1520-510X ; 0020-1669
    ISSN (online) 1520-510X
    ISSN 0020-1669
    DOI 10.1021/acs.inorgchem.3c01982
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  2. Article ; Online: Os(II)-Bridged Polyarginine Conjugates: The Additive Effects of Peptides in Promoting or Preventing Permeation in Cells and Multicellular Tumor Spheroids.

    Gkika, Karmel S / Noorani, Sara / Walsh, Naomi / Keyes, Tia E

    Inorganic chemistry

    2021  Volume 60, Issue 11, Page(s) 8123–8134

    Abstract: The preparation of two polyarginine conjugates of the complex Os(II) [bis-(4'-(4-carboxyphenyl)-2,2':6',2″-terpyridine)] [Os-( ... ...

    Abstract The preparation of two polyarginine conjugates of the complex Os(II) [bis-(4'-(4-carboxyphenyl)-2,2':6',2″-terpyridine)] [Os-(R
    MeSH term(s) Animals ; Antineoplastic Agents/chemical synthesis ; Antineoplastic Agents/chemistry ; Antineoplastic Agents/pharmacology ; Cell Membrane Permeability/drug effects ; Cell Proliferation/drug effects ; Cell Survival/drug effects ; Cells, Cultured ; Coordination Complexes/chemical synthesis ; Coordination Complexes/chemistry ; Coordination Complexes/pharmacology ; Cricetulus ; Drug Screening Assays, Antitumor ; Humans ; Molecular Structure ; Optical Imaging ; Osmium/chemistry ; Osmium/pharmacology ; Peptides/chemistry ; Peptides/pharmacology ; Spheroids, Cellular/drug effects
    Chemical Substances Antineoplastic Agents ; Coordination Complexes ; Peptides ; polyarginine (25212-18-4) ; Osmium (2E7M255OPY)
    Language English
    Publishing date 2021-05-12
    Publishing country United States
    Document type Journal Article
    ZDB-ID 1484438-2
    ISSN 1520-510X ; 0020-1669
    ISSN (online) 1520-510X
    ISSN 0020-1669
    DOI 10.1021/acs.inorgchem.1c00769
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  3. Article ; Online: Synthesis and Pro-Apoptotic Effects of Nitrovinylanthracenes and Related Compounds in Chronic Lymphocytic Leukaemia (CLL) and Burkitt's Lymphoma (BL).

    Byrne, Andrew J / Bright, Sandra A / McKeown, James P / Bergin, Adam / Twamley, Brendan / McElligott, Anthony M / Noorani, Sara / Kandwal, Shubhangi / Fayne, Darren / O'Boyle, Niamh M / Williams, D Clive / Meegan, Mary J

    Molecules (Basel, Switzerland)

    2023  Volume 28, Issue 24

    Abstract: Chronic lymphocytic leukaemia (CLL) is a malignancy of the immune B lymphocyte cells and is the most common leukaemia diagnosed in developed countries. In this paper, we report the synthesis and antiproliferative effects of a series of ( ...

    Abstract Chronic lymphocytic leukaemia (CLL) is a malignancy of the immune B lymphocyte cells and is the most common leukaemia diagnosed in developed countries. In this paper, we report the synthesis and antiproliferative effects of a series of (
    MeSH term(s) Humans ; Burkitt Lymphoma/drug therapy ; Burkitt Lymphoma/metabolism ; Burkitt Lymphoma/pathology ; Leukemia, Lymphocytic, Chronic, B-Cell/drug therapy ; Leukemia, Lymphocytic, Chronic, B-Cell/pathology ; B-Lymphocytes/metabolism ; Cell Line ; Anthracenes
    Chemical Substances Anthracenes
    Language English
    Publishing date 2023-12-14
    Publishing country Switzerland
    Document type Journal Article
    ZDB-ID 1413402-0
    ISSN 1420-3049 ; 1431-5165 ; 1420-3049
    ISSN (online) 1420-3049
    ISSN 1431-5165 ; 1420-3049
    DOI 10.3390/molecules28248095
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    In stock of ZB MED Cologne/Königswinter

    Zs.MO 81: Show issues

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  4. Article: Synthesis and Biological Evaluation of 1-(Diarylmethyl)-1

    Ana, Gloria / Kelly, Patrick M / Malebari, Azizah M / Noorani, Sara / Nathwani, Seema M / Twamley, Brendan / Fayne, Darren / O'Boyle, Niamh M / Zisterer, Daniela M / Pimentel, Elisangela Flavia / Endringer, Denise Coutinho / Meegan, Mary J

    Pharmaceuticals (Basel, Switzerland)

    2021  Volume 14, Issue 2

    Abstract: We report the synthesis and biochemical evaluation of compounds that are designed as hybrids of the microtubule targeting benzophenone phenstatin and the aromatase inhibitor letrozole. A preliminary screening in estrogen receptor (ER)-positive MCF-7 ... ...

    Abstract We report the synthesis and biochemical evaluation of compounds that are designed as hybrids of the microtubule targeting benzophenone phenstatin and the aromatase inhibitor letrozole. A preliminary screening in estrogen receptor (ER)-positive MCF-7 breast cancer cells identified 5-((2
    Language English
    Publishing date 2021-02-22
    Publishing country Switzerland
    Document type Journal Article
    ZDB-ID 2193542-7
    ISSN 1424-8247
    ISSN 1424-8247
    DOI 10.3390/ph14020169
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  5. Article ; Online: β-Lactams with antiproliferative and antiapoptotic activity in breast and chemoresistant colon cancer cells.

    Malebari, Azizah M / Fayne, Darren / Nathwani, Seema M / O'Connell, Fiona / Noorani, Sara / Twamley, Brendan / O'Boyle, Niamh M / O'Sullivan, Jacintha / Zisterer, Daniela M / Meegan, Mary J

    European journal of medicinal chemistry

    2020  Volume 189, Page(s) 112050

    Abstract: A series of novel 1,4-diaryl-2-azetidinone analogues of combretastatin A-4 (CA-4) have been designed, synthesised and evaluated in vitro for antiproliferative activity, antiapoptotic activity and inhibition of tubulin polymerisation. Glucuronidation of ... ...

    Abstract A series of novel 1,4-diaryl-2-azetidinone analogues of combretastatin A-4 (CA-4) have been designed, synthesised and evaluated in vitro for antiproliferative activity, antiapoptotic activity and inhibition of tubulin polymerisation. Glucuronidation of CA-4 by uridine 5-diphosphoglucuronosyl transferase enzymes (UGTs) has been identified as a mechanism of resistance in cancer cells. Potential sites of ring B glucuronate conjugation are removed by replacing the B ring meta-hydroxy substituent of selected series of β-lactams with alternative substituents e.g. F, Cl, Br, I, CH
    MeSH term(s) Antineoplastic Agents/chemical synthesis ; Antineoplastic Agents/metabolism ; Antineoplastic Agents/pharmacology ; Apoptosis/drug effects ; Binding Sites ; Cell Line, Tumor ; Cell Proliferation/drug effects ; Drug Screening Assays, Antitumor ; G2 Phase Cell Cycle Checkpoints/drug effects ; HEK293 Cells ; Humans ; Microsomes, Liver/metabolism ; Molecular Docking Simulation ; Molecular Structure ; Necrosis/chemically induced ; Protein Binding ; Stilbenes/chemistry ; Survivin/metabolism ; Tubulin/metabolism ; Tubulin Modulators/chemical synthesis ; Tubulin Modulators/metabolism ; Tubulin Modulators/pharmacology ; beta-Lactams/chemical synthesis ; beta-Lactams/metabolism ; beta-Lactams/pharmacology
    Chemical Substances Antineoplastic Agents ; Stilbenes ; Survivin ; Tubulin ; Tubulin Modulators ; beta-Lactams ; fosbretabulin (I5590ES2QZ)
    Language English
    Publishing date 2020-01-10
    Publishing country France
    Document type Journal Article
    ZDB-ID 188597-2
    ISSN 1768-3254 ; 0009-4374 ; 0223-5234
    ISSN (online) 1768-3254
    ISSN 0009-4374 ; 0223-5234
    DOI 10.1016/j.ejmech.2020.112050
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    In stock of ZB MED Cologne/Königswinter

    Zs.B 784: Show issues Location:
    Je nach Verfügbarkeit (siehe Angabe bei Bestand)
    bis Jg. 2021: Bestellungen von Artikeln über das Online-Bestellformular
    ab Jg. 2022: Lesesaal (EG)

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  6. Article ; Online: Synthesis and evaluation of antiproliferative microtubule-destabilising combretastatin A-4 piperazine conjugates.

    O'Boyle, Niamh M / Ana, Gloria / Kelly, Patrick M / Nathwani, Seema M / Noorani, Sara / Fayne, Darren / Bright, Sandra A / Twamley, Brendan / Zisterer, Daniela M / Meegan, Mary J

    Organic & biomolecular chemistry

    2019  Volume 17, Issue 25, Page(s) 6184–6200

    Abstract: Microtubules are a validated clinical target for the treatment of many cancers. We describe the design, synthesis, biochemical evaluation, and molecular modelling studies of a series of analogues of the microtubule-destabilising agent, combretastatin A-4 ...

    Abstract Microtubules are a validated clinical target for the treatment of many cancers. We describe the design, synthesis, biochemical evaluation, and molecular modelling studies of a series of analogues of the microtubule-destabilising agent, combretastatin A-4 (CA-4). Our series of 33 novel compounds contain the CA-4 core structure with modifications to the stilbene linking group, and are predominantly piperazine derivatives. Synthesis was achieved in a two-step process by firstly obtaining the acrylic acid via a Perkin reaction using microwave enhanced synthesis, followed by coupling using either DCC or Mukaiyama's reagent. All target compounds were screened for antiproliferative activity in MCF-7 breast cancer cells. Hydroxyl derivative (E)-3-(4-hydroxy-3-methoxyphenyl)-1-(4-phenylpiperazin-1-yl)-2-(3,4,5-trimethoxyphenyl) propenone (4m) displayed potent antiproliferative activity (IC50 = 190 nM). Two amino-containing derivatives, (E)-3-(3-amino-4-methoxyphenyl)-1-(4-phenylpiperazin-1-yl)-2-(3,4,5-trimethoxyphenyl)prop-2-en-1-one (4q) and (E)-3-(3-amino-4-methoxyphenyl)-1-(4-(p-tolyl)piperazin-1-yl)-2-(3,4,5-trimethoxyphenyl)prop-2-en-1-one (4x), were the most potent with IC50 values of 130 nM and 83 nM respectively. Representative compounds were shown to depolymerise tubulin, induce G2/M arrest and apoptosis in MCF-7 cells but not peripheral blood mononuclear cells, and induce cleavage of the DNA repair enzyme poly ADP ribose polymerase (PARP) in MCF-7 cells. Modelling studies predict that the compounds bind to tubulin within the colchicine-binding site. These compounds are a valuable addition to the library of CA-4 analogues and 4m, 4q and 4x will be developed further as novel, water-soluble molecules targeting microtubules.
    MeSH term(s) Antineoplastic Agents/chemical synthesis ; Antineoplastic Agents/metabolism ; Antineoplastic Agents/pharmacology ; Apoptosis/drug effects ; Binding Sites ; Drug Screening Assays, Antitumor ; G2 Phase Cell Cycle Checkpoints/drug effects ; Humans ; MCF-7 Cells ; Molecular Docking Simulation ; Piperazines/chemical synthesis ; Piperazines/metabolism ; Piperazines/pharmacology ; Poly(ADP-ribose) Polymerases/metabolism ; Protein Binding ; Stilbenes/chemical synthesis ; Stilbenes/metabolism ; Stilbenes/pharmacology ; Tubulin/chemistry ; Tubulin/metabolism ; Tubulin Modulators/chemical synthesis ; Tubulin Modulators/metabolism ; Tubulin Modulators/pharmacology
    Chemical Substances Antineoplastic Agents ; Piperazines ; Stilbenes ; Tubulin ; Tubulin Modulators ; Poly(ADP-ribose) Polymerases (EC 2.4.2.30) ; fosbretabulin (I5590ES2QZ)
    Language English
    Publishing date 2019-06-07
    Publishing country England
    Document type Journal Article ; Research Support, Non-U.S. Gov't
    ZDB-ID 2097583-1
    ISSN 1477-0539 ; 1477-0520
    ISSN (online) 1477-0539
    ISSN 1477-0520
    DOI 10.1039/c9ob00558g
    Database MEDical Literature Analysis and Retrieval System OnLINE

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