Browsing by Author "Zisterer, Daniela"
Now showing items 1-20 of 20
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3-Vinylazetidin-2-Ones: Synthesis, antiproliferative and tubulin destabilizing activity in MCF-7 and MDA-MB-231 Breast Cancer Cells
Zisterer, Daniela (MDPI, 2019)Microtubule-targeted drugs are essential chemotherapeutic agents for various types of cancer. A series of 3-vinyl-β-lactams (2-azetidinones) were designed, synthesized and evaluated as potential tubulin polymerization ... -
Beta-Lactam Estrogen Receptor Antagonists and a Dual-Targeting Estrogen Receptor/Tubulin Ligand
O'Boyle, Niamh; Zisterer, Daniela; Meegan, Mary (2014) -
Development of novel pyrrolo-1,5-benzoxazepines as anti-cancer agents for the treatment of chronic myeloid leukaemia
Bright, Sandra A. (Trinity College (Dublin, Ireland). School of Biochemistry and Immunology, 2010)Chronic myeloid leukaemia (CML) is characterised by the presence of a constitutively active tyrosine kinase known as Bcr-Abl. The Bcr-Abl kinase inhibitor, STI571, is the first line treatment for CML, but the recent emergence ... -
Enantioseparation and structural optimisation of b-lactams and stilbene analogues for the treatment of triple negative breast and chemoresistant colorectal cancers
McLoughlin, Eavan Ciara (Trinity College Dublin. School of Pharmacy & Pharma. Sciences. Discipline of Pharmacy, 2023)Triple negative breast cancer (TNBC) is characterised by an extremely aggressive clinical phenotype and minimal expression of typical breast cancer receptors such as the estrogen, progesterone or HER2 receptors.1, 2 Patient ... -
Evaluation of the anti-cancer effects of novel pyrrolo-1, 5-benzoxazepines in neuroblastoma
Lennon, Jennifer (Trinity College (Dublin, Ireland). School of Biochemistry and Immunology, 2015)Neuroblastoma, a malignancy of neuroectodermal origin, accounts for 15% of childhood cancer deaths. Despite both advances in understanding the biology of the cancer and aggressive treatment strategies, it continues to be ... -
Investigation into the mechanism by which a novel series of pyrrolo-1,5-benzoxazepine compounds induce apoptosis in chronic myelogenous leukaemia cells
McGee, Margaret (Trinity College (Dublin, Ireland). School of Biochemistry and Immunology, 2001)Some members of a novel series of pyrrolo-1,5-benzoxazepine compounds induce apoptosis in human chronic myeloid leukaemia (CML) cells. A representative compound, PBOX-6, induces apoptosis in a dose- and time-dependent ... -
Investigation into the mechanism underlying the antiproliferative and apoptotic effects of pyrrolo-1,5-benzoxazepine compounds
Mulligan, Jude (Trinity College (Dublin, Ireland). School of Biochemistry and Immunology, 2004)A novel series of pyrrolo-1,5-benzoxazepine (PBOX) compounds have potential as anti-cancer agents. The PBOX compounds appear to be subdivided into two groups, those that exert antiproliferative effects (e.g. PBOX-21) by ... -
Investigation into the Molecular Mechanisms Underlying Chemoresistance in Malignant Rhabdoid Tumours
Hannon Barroeta, Patricia (Trinity College Dublin. School of Biochemistry & Immunology. Discipline of Biochemistry, 2023)Malignant rhabdoid tumour (MRT) is a rare and aggressive paediatric malignancy associated with poor prognosis and is, unfortunately, highly refractive to treatment. One of the major issues when treating MRT patients is the ... -
A Jocic-type approach for a practical and scalable synthesis of pyrrolonaphthoxazepine (PNOX)-based potent proapoptotic agents
Zisterer, Daniela; Federico, Stefano; Khan, Tuhina; Relitti, Nicola; Chemi, Giulia; Brindisi, Margherita; Brogi, Simone; Novellino, Ettore; Campiani, Giuseppe; Gemma, Sandra; Butini, Stefania (2018)We developed a Jocic-type protocol for the construction of the pyrrolonaphthoxazepine (PNOX) core. After an initial investigation based on the isolation of a trichloromethyl carbinol derivative, we shifted our attention ... -
Lead Optimization of Benzoxepin-Type Selective Estrogen Receptor (ER) Modulators and Downregulators with Subtype-Specific ER-alpha and ER-beta Activity
O'Boyle, Niamh; Meegan, Mary; Zisterer, Daniela; Fayne, Darren (2018) -
Piperlongumine (piplartine) and analogues: Antiproliferative microtubule-destabilising agents.
Zisterer, Daniela; O'Boyle, Niamh; Meegan, Mary (2017) -
Raising the bar in anticancer therapy:recent advances in, and perspectives on, telomerase inhibitors
Zisterer, Daniela; Saraswati, A Prasanth; Relitti, Nicola; Brindisi, Margherita; Gemma, Sandra; Butini, Stefania; Campiani, Giuseppe (2019)Telomerase is a ribonucleic reverse transcriptase enzyme that uses an integral RNA component as a template to add tandem telomeric DNA repeats, TTAGGG, at the 3′ end of the chromosomes. 85–90% of human tumors and their ... -
Spiroindoline-Capped Selective HDAC6 Inhibitors: Design, 2 Synthesis, Structural Analysis, and Biological Evaluation
Zisterer, Daniela; Kelly, Vincent; O'Sullivan, Jeffrey (2020)Histone deacetylase inhibitors (HDACi) have emerged as promising therapeutics for the treatment of neurodegeneration, cancer, and rare disorders. Herein, we report the development of a series of spiroindoline-based HDAC6 ... -
Structure-activity relationships, biological evaluation and structural studies of novel pyrrolonaphthoxazepines as antitumor agents
Zisterer, Daniela; O'Sullivan, Jeffrey; Brindisi, Margherita; Ulivieri, Cristina; Alfano, Gloria; Gemma, Sandra; de Asís Balaguer, Francisco; Khan, Tuhina; Grillo, Alessandro; Chemi, Giulia; Menchon, Grégory; Prota, Andrea E.; Olieric, Natacha; Lucena-Agell, Daniel; Barasoain, Isabel; Fernando Diaz, J.; Nebbioso, Angela; Conte, Mariarosaria; Lopresti, Ludovica; Magnano, Stefania; Amet, Rebecca; Kinsella, Paula; Ibrahim, Ola; Morbidelli, Lucia; Spaccapelo, Roberta; Baldari, Cosima; Butini, Stefania; Novellino, Ettore; Campiani, Giuseppe; Altucci, Lucia; Steinmetz, Michel O.; Brogi, Simone (2019)Microtubule-targeting agents (MTAs) are a class of clinically successful anti-cancer drugs. The emergence of multidrug resistance to MTAs imposes the need for developing new MTAs endowed with diverse mechanistic properties. ...