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Showing 1 to 20 of 68 for “"Taxol"”.
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Studies on water-soluble taxol derivatives
The importance of taxol as an anticancer drug lies not only in its activity in antitumor assays but also in its unique mechanism of action. Unfortunately, taxol is not water-soluble and therefore must be given in conjunction with emulsifying agents. Modifications of taxol were carried out in order …
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Studies on the chemistry of taxol
The novel diterpenoid taxol isolated from the western yew Taxus brevifolia is one of the most important lead compounds to emerge from the search for anticancer agents from plants. It shows consistent clinical activity against ovarian cancer and may also be active against other cancers. In this …
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Investigations of the chemistry of taxol
Several C-7 and C-13 diazirinyl taxol analogs have been synthesized as potential photoaffinity-labeled derivatives for studying the nature of the binding site of taxol on polymerized tubulin. One analog has been prepared in both deuterium- and tritium-labeled versions. Methods were developed to …
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Assessment of taxol activity: Bioavailability in human physiological fluids and QSAR of taxol analogues based on a neural network design
Taxol is an anticancer agent that is highly protein bound. This feature is addressed in the first chapter by developing a competitive, enzyme-linked immunosorbent assay (ELISA) to quantify bioavailability of taxol in human fluids: plasma, plasma ultrafiltrate and salivary fluids. An optimization …
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Synthesis of Taxol™ Analogs as Conformational Probes
Taxol™, isolated from the bark of Taxus brevifolia in the late 1960s, and the semisynthetic analog Taxotere™ have proven clinical importance for the treatment of ovarian and breast cancer. Taxol™ exerts its biological effect by binding to polymerized tubulin and stabilizing the resulting …
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Studies on Taxol Resistance Induced by HBx Viral Oncoprotein
… the effective chemotherapeutic potential of taxol has been shown in a variety ofcancers such as ovarian,breast and lung.However,chemotherapy with taxol often fails due to resistance of hepatocellular carcinoma (HCC). I attempted to determine the effect of taxolon HCC.Infection with hepatitis …
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A New Synthesis of Taxol®, from Baccatin III
Taxol®, an important anticancer drug, was first isolated in extremely low yield from the bark of the western yew, Taxus brevifolia. The clinical utility of Taxol has prompted a tremendous effort to obtain this complex molecule synthetically. Due to the chemical complexity of Taxol, its commercial …
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Syntheses and Bioactivities of Targeted and Conformationally Restrained Taxol Analogs
Taxol (1) was first isolated from the bark of the Pacific yew about 35 years ago by Drs. Wall and Wani. Although its development as an anticancer agent was delayed by numerous reasons, including its scarcity and insolubility, the discovery of its tubulin-assembly activity and other factors …
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Chemical studies of the C-4 position of baccatin III and taxol
Because of the efficacy of taxol against a wide variety of cancers, the demand for this drug has vastly increased during the last decade. Due to its limited natural supply, a number of alternative sources of taxol continue to be investigated. One approach toward alleviating the taxol supply problem …
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Isolation, structure elucidation and approaches to the partial synthesis of new taxol analogs
… the source of the important anticancer drug taxol, but it also contains many other natural taxoids. These compounds are of interest both from a structural viewpoint and also as a starting point for the synthesis of paclitaxel analogs. As a complement to our ongoing studies on the chemistry of …
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Synthesis and biological studies of a fullerene-Taxol conjugate and fullerene-based transfection vectors
… of lipophilic chemotherapeutics to lung cancer. TaxolRTM (paclitaxel), one of the most active anticancer drugs in clinical use, has shown significant potential for treatment of lung cancer when delivered by the liposome aerosol method. However, rapid clearance of Taxol from the lungs (within 40 …
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Construction of carbocycles via oxonium ylides generation and rearrangement: towards the synthesis of taxol
The diterpenoid natural product Taxol, first discovered in the late 1960’s, is one of the most important current drugs for the treatment of several cancers including breast and ovarian cancers. Although tremendous efforts towards its synthesis have been made in the last two decades, resulting in …
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The chemistry of cephalomannine
… closely related to the potent anticancer agent Taxol. Three aspects of its chemistry were examined. First, cephalomannine was converted to Taxol. This conversion was accomplished by the reaction of a 2'- benzoyl-7-Troc cephalomannine/Taxol mixture with oxalyl chloride to generate a common oxamic …
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New methodology for the generation and cycloadditions of thio-substituted ketenes ; A synthetic approach to the taxol A-ring
Thesis (Ph. D.)--Massachusetts Institute of Technology, Dept. of Chemistry, 1997.
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Evaluating local skin heating as an early detection method for small-fiber neuropathy in women with breast cancer receiving paclitaxel (Taxol®)
… survivors (BCS) during the first 6 weeks of Taxol®. Aims of the study were to compare the mean size of (1) axon reflexes and (2) axon flares (both markers of small fiber nerve function) in BCS receiving Taxol® to the size of reflexes/flares in healthy female controls (HCs). A third aim was to …
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Modified taxols as anticancer agents
Modifications of the potent anticancer agent taxol were carried out in order to gain an understanding of the chemical reactivity of the drug and the factors which contribute to its biological activity. The C-2' and/or the C-7 hydroxyl groups of taxol were substituted with acetyl, ßalanyl, silyl, …
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Syntheses and Bioactivities of Targeted and Conformationally Restrained Paclitaxel and Discodermolide Analogs
… this work, the synthesis of isotopically labeled taxol analogs is described and the REDOR studies of this compound complexed to tubulin agrees with the hypothesis that palictaxel adopts T-taxol conformation. Based on T-taxol conformation, macrocyclic analogs of taxol have been prepared and their …
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Design, Syntheses and Biological Activities of Paclitaxel Analogs
… on the protein has been proposed to be the T-taxol conformation, and paclitaxel analogs constrained to the T-taxol conformation proved to be significantly more active than paclitaxel in both cytotoxicity and tubulin polymerization assays, thus validating the T-taxol conformation as the …
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Approaches to the synthesis of modified taxols
… on the synthesis of the C-13 side chain of taxol was carried out in order to prepare modified taxol derivatives by coupling of the side chain acid chloride to a suitably protected baccatin III. The side chain was prepared by the Darzens condensation. Acylation of baccatin III was performed …
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Experimental and Computational Studies in Bioorganic and Synthetic Organic Chemistry
… approach, we synthesized Taxol-based dimer in which the baccatin III core of Taxol is coupled with flexible PEG linker. However, microtubule assembly assay suggested that these new dimers are not capable of effecting bivalent binding to the Taxol binding sites in …
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