Preparation and biological activity of taxol acetates

Mellado, Wilfredo; Magri, Neal F.; Kingston, David G. I.; Garcia-Arenas, Renee; Orr, George A.; Horwitz, Susan Band

doi:10.1016/0006-291x(84)91557-2

Cited by 96 publications

(68 citation statements)

References 9 publications

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“…They gave a single spot on TLC plates with several eluents. [Mellado et al, 1984] by its conversion into 2Ј-O-acetyl-7-O-(L-alanyl)taxol and subsequent reaction with 4Ј-carboxyfluorescein succinimidyl ester (Molecular Probes C-2210, Eugene, OR). N-(4Ј-fluoresceincarbonyl)-L-alanine methyl ester was prepared by the reaction of the same succinimidyl ester with L-alanine methyl ester hydrochloride (Fluka 05200, Buchs, Switzerland).…”

Section: Materials and Methods Fluorescent Taxoids And Other Materialsmentioning

confidence: 99%

Fluorescent taxoids as probes of the microtubule cytoskeleton

Evangelio

Abal

Barasoaín

et al. 1998

Cell Motil. Cytoskeleton

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Section: Materials and Methods Fluorescent Taxoids And Other Materialsmentioning

confidence: 99%

Fluorescent taxoids as probes of the microtubule cytoskeleton

Evangelio

Abal

Barasoaín

et al. 1998

Cell Motil. Cytoskeleton

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“…The authors confirmed the formation of a 2’- O -substituted paclitaxel derivative by the characteristic downfield shifts in the 1 H- and 13 C-NMR of the signals of H-C(2’) from δ(H) 4.77 [91] to 5.50 and of C(2’) from δ(C) 73.2 [91] to 74.2, respectively.…”

Section: Synthesis and Applications Of Ha-paclitaxel Bioconjugatementioning

confidence: 75%

“…Joining a bioactive compound to a biocompatible polymer offers, in general, several advantages like better drug solubilization, stabilization, localization and controlled release [88,89,90]. For derivatives other than those quoted above, see [91,92,93,94,95,96,97,98,99,100]. …”

Section: Introductionmentioning

confidence: 99%

Design, Synthesis and Applications of Hyaluronic Acid-Paclitaxel Bioconjugates†

et al. 2008

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Paclitaxel (1a), a well known antitumor agent adopted mainly for the treatment of breast and ovarian cancer, suffers from significant disadvantages such as low solubility, certain toxicity and specific drug-resistance of some tumor cells. To overcome these problems extensive research has been carried out. Among the various proposed strategies, the conjugation of paclitaxel (1a) to a biocompatible polymer, such as hyaluronic acid (HA, 2), has also been considered. Coupling a bioactive compound to a biocompatible polymer offers, in general, many advantages such as better drug solubilization, better stabilization, specific localization and controlled release. Hereafter the design, synthesis and applications of hyaluronic acid-paclitaxel bioconjugates are reviewed. An overview of HA-paclitaxel combinations is also given.

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“…These conjugates were tested in a tubulin assembly assay and evaluated for their cytotoxicities against human mammary cancer cell line MCF7. In the tubulin assembly assay, the C7 and C10 conjugates ( the hydroxyl group at the C2 0 position was crucial to maintain the tubulin assembly activity of paclitaxel [72]. In the cytotoxicity assay, all these compounds were less potent than paclitaxel.…”

Section: New Chemistry Of Paclitaxelmentioning

confidence: 99%