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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 20 of 24 for “"Tubulin polymerization."”.
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Sulforaphane Inhibits Mammary Cancer Cell Mitotic Progression and Tubulin Polymerization
… spindles, and higher doses of SUL inhibited tubulin polymerization in vitro. In addition, BALB/c mice injected s.c. with F3II cells and subsequently injected daily i.v. with SUL (15 nmol/day for 13 days) developed significantly smaller tumors (∼60% less in mass) than vehicle-treated …
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Discovery of Novel Tubulin Polymerization Inhibitors and Survivin Inhibitors as Potential Anticancer Agents
… by targeting two important cancer targets: tubulin and survivin. Microtubules play important role in mitosis and cell division. Cancer cells divide more rapidly than normal cells, and thus are more sensitive to tubulin targeting agents which disrupt mitosis. Targeting tubulin for anticancer …
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Discovery of Inhibitors of Inhibitors of Apoptosis Proteins and Novel Tubulin Polymerization Inhibitors as Potential Anticancer Agents
… important cancer targets: survivin, MDM2, and tubulin. Survivin, a member of the inhibitor of apoptosis proteins (IAPs) family, serves as both an apoptosis suppressor and a pivotal player in cell division. Its significance as a cancer drug target arises from its heightened expression in various …
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Design and synthesis of indole-based analogues of OXi8006 as inhibitors of tubulin polymerization and their incorporation as payloads in drug-linker constructs.
… University, exhibited potent inhibition of tubulin polymerization and strong cytotoxicity against human various cancer cell lines. In previous studies, OXi8007, the phosphate prodrug of OXi8006, demonstrated vascular disrupting activity within 2 hours of administration by targeting tumor …
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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.
… collaborations) of small-molecule inhibitors of tubulin polymerization and development of targeting strategies that facilitate selective delivery of therapeutic agents to tumors and the tumor microenvironment. The tubulin-microtubule protein has been established as a prime target for anti-cancer …
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Synthesis and biological evaluation of structurally diverse indole-based analogues as inhibitors of tubulin polymerization and synthesis of drug-linker constructs cleavable by enzymes present in the tumor microenvironment.
A sub-set of inhibitors of tubulin polymerization that bind to the colchicine site demonstrate dual functionality as both potent cytotoxins (antiproliferative agents) and effective vascular disrupting agents (VDAs). Our previous studies led to the discovery of a potent inhibitor of tubulin …
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The Substrate and Regulator of Acetyltransferase San
… affinity purification and demonstrated that tubulin is a San substrate. Tubulins are the building blocks of microtubules, which display dynamic instability. By regulating the rate of microtubule assembly and disassembly, cells organize the microtubule cytoskeleton to accommodate their …
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In vitro anti-cancer effects of benzimidazoles on the canine osteosarcoma D17 cell line
… death. Soluble VEGF secretion and the effect on tubulin polymerization were also evaluated in vitro. Specifically, the in vitro effects of ABZ, FBZ and MBZ on D17 canine OS cells were investigated by characterizing 1) cell proliferation with an MTS assay, 2) apoptosis via flow cytometry, 3) VEGF …
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Syntheses and Bioactivities of Targeted and Conformationally Restrained Paclitaxel and Discodermolide Analogs
… It exerts its biological effect by promoting tubulin polymerization and stabilizing the resulting microtubules. Paclitaxel has become one of the most important current drugs for the treatment of breast and ovarian cancers. Studies aimed at understanding the biologically active conformation of …
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Discovery of Pyrimidine-based Heterocycles as Single Agents With Combination Chemotherapy Potential And As Inhibitors Of Purine Nucleotide Biosynthesis For The Treatment of Cancer
… features that are necessary for inhibition of tubulin polymerization as well as for inhibition of one or more of the receptor tyrosine kinases (RTKs)- vascular endothelial growth factor receptor-2 (VEGFR2), platelet derived growth factor receptor-β (PDGFRβ) and epidermal growth factor receptor …
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Design, synthesis, and biological evaluation of dihydronaphthalene and chalcone-based anticancer agents inspired by the natural product combretastatin A-4.
… as vascular disrupting agents (VDAs), affect the tubulin dynamics of endothelial cells lining tumor-associated blood vessels. Tubulin depolymerization causes the endothelial cells to change shape and detach from the vessel wall leading to vessel collapse, which ultimately results in tumor …
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The chemistry of cephalomannine
… synthetically prepared for testing in several tubulin polymerization systems. Earlier studies had shown that some Taxol analogs had the ability to stabilize tubulin polymers to cold, but failed to induce assembly as does Taxol. The compounds prepared were used to investigate the differences and …
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Syntheses and Bioactivities of Targeted and Conformationally Restrained Taxol Analogs
… scarcity and insolubility, the discovery of its tubulin-assembly activity and other factors motivated oncologists to overcome these problems. It has since become one of the most important current drugs for the treatment of several cancers, including breast and ovarian cancers. Like almost all …
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Synthesis and evaluation of novel antivascular agents for two-photon activation
… Combretum caffrum. These agents interact with tubulin in a similar way to colchicine, causing destruction of blood vessels within tumours by binding to tubulin dimers and inhibiting angiogenesis in developing tumours. Cis-combretastatins are effective chemotherapeutic agents showing potent …
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Design and Synthesis of Pyrimidine Fused Heterocycles as Single Agents with Combination Chemotherapy Potential
… features that are necessary for inhibition of tubulin polymerization. Structural modifications also led to the identification of novel antiangiogenic agents which inhibit one or more of the receptor tyrosine kinases (RTKs)– vascular endothelial growth factor receptor–2 (VEGFR2), platelet …
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Inhibitors of tubulin, nitric oxide synthase, and HIF-1 alpha; synthesis, biological, and biochemical evaluation.
… cancer cytotoxicity and their ability to inhibit tubulin polymerization. The 3′-amino stilbene 15 was the most effective of the fluoro-nitro stilbenes synthesized, having a tubulin IC50 of 2.9 µM, and a cell cytotoxicity of 0.0093 µg/mL against NCI H460 lung cancer carcinoma. Though VDAs have been …
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Design, Syntheses and Biological Activities of Paclitaxel Analogs
… active than paclitaxel in both cytotoxicity and tubulin polymerization assays, thus validating the T-taxol conformation as the tubulin-binding conformation. In this work, eight compounds containing an aza-tricyclic moiety as a mimic of the baccatin core of paclitaxel have been designed and …
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Design and Synthesis of Pyrimidine Based Heterocycles as Potential Anti-cancer Agents with Combination Chemotherapeutic Potential or Targeted One Carbon Metabolism Inhibition and Anti-opportunistic Agents
… features that are necessary for inhibition of tubulin polymerization or thymidylate synthase as well as for inhibition of one or more of the receptor tyrosine kinases (RTKs)- vascular endothelial growth factor receptor-2 (VEGFR2), epidermal growth factor receptor (EGFR) and/or platelet-derived …
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Design and synthesis of pyrimido[4,5-b]indoles and furo[2,3-d]pyrimidines as single agents with combination chemotherapy potential or as inhibitors of tubulin or thymidylate synthase
… in the areas of multitargeted single agents and tubulin inhibitors in cancer chemotherapy and selective Toxoplasma gondii TS inhibitors for the treatment of toxoplasmosis.</p><p> Tubulin inhibitors are important antitumor agents that disrupt microtubule dynamics. Thymidylate synthase (TS) …
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DEVELOPMENT OF MOLECULAR PROBES ACTING ON aSYN/TUBULIN AND TAU/TUBULIN INTERACTION
… to mammals mainly consisting of conserved α/β tubulin heterodimers. Neurons are an impressive example of cells in which the contribution of MTs is fundamental to achieve their sophisticated cell architecture and to sustain their functional complexity. A growing body of evidence indicates that …
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