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Search theses and dissertations gathered from participating repositories worldwide. Every result links back to the library that holds it. No account is needed.
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Showing 1 to 13 of 13 for “"Combretastatin A-4."”.
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Synthesis and evaluation of tetramethoxy stilbenes related to combretastatin A-4 as potential anticancer agents
… display less toxicity (Ali et al., 2012). Combretastatins are known to have cytotoxic activity against cancer cells with minimal side effects (Kretzschmann & Fürst, 2013). Derivatives with improved activity and less detrimental side effects are required. The different activities of …
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Biochemical studies of targeted and bimodal analogues of the natural anticancer compounds combretastatin A-4 and illudin M
This thesis presents a study on novel chemotherapeutics based on naturally designed scaffolds. The cytotoxicity of promising pharmaceutical compounds was tested on various cells of neural and/or cancerous origin, monitoring their specificity, re-growth retardation and mechanism of apoptosis …
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Design, synthesis, and biological evaluation of dihydronaphthalene and chalcone-based anticancer agents inspired by the natural product combretastatin A-4.
… results in tumor necrosis. The natural product combretastatin A-4 (CA4) is widely accepted as the gold standard of VDAs and the clinical success of its corresponding water-soluble phosphate prodrug salt CA4P has inspired the development of a myriad of analogues and derivatives. Two …
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Synthesis and evaluation of novel heterocyclic compounds as anticancer agents
… and tubulin sulfhydryl binding sites. Combretastatin A-4 is one of the mostpotent natural products targeting tubulin and prevents microtubule polymerisation thatleads to mitosis arrest and apoptosis in endothelial cells. Moreover, it can cause selectivevascular shutdown for the tumour …
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Design and synthesis of dihydronaphthalene vascular disrupting agents and indolequinone-based bioreductives.
… show great promise. The naturally occurring combretastatins, especially combretastatin A-4 (CA4) and combretastatin A-1 (CA1), in suitable prodrug form, have proven to be highly effective VDAs. In this study, efforts were directed towards the synthesis of two combretastatin analogs bearing …
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Development of novel heterocyclic compounds as vascular targeting agents
… of a series of simple biaryl compounds and Combretastatin A-4.
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Targeting the tumor microenvironment through the design and synthesis of potent, small-molecule, anticancer agents.
… treatment of cancer. With the discovery of the combretastatin extended family of compounds in the late 1970's and early 80's, there has been an accelerated interest in vascular targeting as a possible cancer treatment methodology. Two natural products, combretastatin A-1 (CA1) and combretastatin …
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Design and synthesis of benzosuberene and tetracyclic-based molecules inspired by natural products as inhibitors of tubulin polymerization and preparation of drug-linker constructs to facilitate tumor selective targeted delivery.
… clinical relevance. Natural products such as combretastatin A-4 and colchicine that bind to the colchicine site (functioning as potent inhibitors of tubulin polymerization and antiproliferative agents) have been evaluated clinically and have inspired countless analogues and derivatives. The …
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Investigation of protein induction in vascular-targeted strategies.
… tumour vascular disrupting agent, combretastatin A-4-phosphate (CA-4-P) have been studied. The gross haemorrhagic pharmacological response elicited by CA-4-P was visible by MALDI-MSI throughout the fibrosarcoma 120 time course. The latter encouraged the prospect that other proteins …
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Etablierung von Methoden zur Bioevaluation antitumoraler Naturstoffe, Metabolite und Analoga
… Einige Derivate der antivaskulären Verbindung Combretastatin A-4 7a wurden mit Hilfe des CAM-Assays untersucht. Die meisten zeigten hierbei erwartungsgemäß ein vergleichbares Verhalten. Besonders interessant ist der Aktivitätsunterschied der Combretastatin-Analoga 26h und 26i. Dieser wurde …
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Synthesis Of 1,4-Triazolyl Combretacoumarins As Potential Anticancer Agents
… making them pharmacologically important. Combretastatin A-4 (CA-4) is a microtubule-binding agent that has potent cytotoxic effects against human cell lines. In CA-4 the trimethoxyarene moiety plays a crucial role in its carcinopreventive effect. Thus, we decided to synthesize novel, …
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Naturstoff-basierte Cytostatika mit verbesserter Tumorselektivität und Potential zur Überwindung von Wirkstoffresistenzen
… sich mit Derivaten des Phase-III-Wirkstoffs Combretastatin A-4 und dem Ziel, die Effizienz sowie die pharmakologischen Eigenschaften zu verbessern. Zur Konjugatsynthese eigneten sich in erster Linie bekannte Chalkon-Analoga. Bemerkenswert ist vor allem ein neues Pt-Konjugat, welches bei …
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A mechanistic assessment of novel anticancer drugs targeting the metastatic cascade and tumour vascularisation.
… derivate Verubulin or the natural drug Combretastatin A-4 (CA-4). Their preclinical evaluation includes the determination of their in vitro cytotoxicity profile against a panel of different tumour cells lines and various biochemical and immunological methods to clarify their molecular …