148930-54-5

Upstream product

• 994-30-9 triethylsilyl chloride 
• 33069-62-4 taxol 
• 219780-99-1 2’-TES-7-TROC-taxol 

Downstream Products

• 149705-82-8 C₅₅H₆₇NO₁₄S₂Si 
• 171781-02-5 C₄₈H₅₀F₃NO₁₆S 
• 220167-85-1 2'-triethylsilyl-7-(tert-butoxycarbonylaminocaproyl)paclitoxel 
• 473912-16-2 2'-(triethylsilyl)-7-[N-(4-methoxytrityl)-β-alanyl]paclitaxel 
• 911051-08-6 C₈₉H₁₀₁NO₂₁Si 
• 1616503-76-4 (2aR,4S,4aS,6R,9S,11S,12S,12bS)-6,12b-bis(acetyloxy)-9-({(2R,3S)-3-(benzoylamino)-3-phenyl-2-[(triethylsilyl)oxy]propanoyl}oxy)-4-(hex-5-ynoyloxy)-11-hydroxy-4a,8,13,13-tetramethyl-5-oxo-2a,3,4,4a,5,6,9,10,11,12,12a,12b-dodecahydro-1H-7,11-methanocyclodeca[3,4]benzo[1,2-b]oxet-12-yl benzoate 
• 1587638-51-4 (2aR,4S,4aS,6R,9S,11S,12S,12bS)-6,12b-bis(acetyloxy)-9-{[(2R,3S)-3-(benzoylamino)-2-hydroxy-3-phenylpropanoyl]oxy}-4-(hex-5-ynoyloxy)-11-hydroxy-4a,8,13,13-tetramethyl-5-oxo-2a,3,4,4a,5,6,9,10,11,12,12a,12b-dodecahydro-1H-7,11-methanocyclodeca[3,4]benzo[1,2-b]oxet-12-yl benzoate 
• 219950-22-8 C₅₈H₇₅N₃O₁₅Si 
• 1581234-58-3 C₅₂H₆₁N₃O₁₅ 
• 186040-52-8 C₆₀H₆₈N₂O₁₈Si 
• 186040-55-1 C₅₀H₅₇N₃O₁₅ 
• 149705-84-0 C₅₃H₆₅NO₁₃Si 
• 149705-85-1 7-deoxypaclitaxel 

Relevant academic research and scientific papers

In Situ Formation of Homogeneous Tellurium Nanodots in Paclitaxel-Loaded MgAl Layered Double Hydroxide Gated Mesoporous Silica Nanoparticles for Synergistic Chemo/PDT/PTT Trimode Combinatorial Therapy

A folic acid (FA) functional drug delivery system (MT?L-PTX?FA) based on in situ formation of tellurium nanodots (Te NDs) in paclitaxel (PTX)-loaded MgAl layered double hydroxide (LDHs) gated mesoporous silica nanoparticles (MSNs) has been designed and fa

Synthesis, biological evaluation and low-toxic formulation development of glycosylated paclitaxel prodrugs

Paclitaxel (PTX) is a famous anti-cancer drug with poor aqueous solubility. In clinical practices, Cremophor EL (polyethoxylated castor oil), a toxic surfactant, is used for dissolution of PTX, which accounts for serious side effects. In the present study

Taxane compound glycosylated derivative and preparation method and application thereof

The invention discloses a taxane compound glycosylated derivative and a preparation method and application thereof. Particularly, the invention relates to a kind of taxane compound glycosylated derivatives, of which the solubility is apparently higher tha

Copper-chelating azides for efficient click conjugation reactions in complex media

The concept of chelation-assisted copper catalysis was employed for the development of new azides that display unprecedented reactivity in the copper(I)-catalyzed azide-alkyne [3+2] cycloaddition (CuAAC) reaction. Azides that bear strong copper-chelating moieties were synthesized; these functional groups allow the formation of azide copper complexes that react almost instantaneously with alkynes under diluted conditions. Efficient ligation occurred at low concentration and in complex media with only one equivalent of copper, which improves the biocompatibility of the CuAAC reaction. Furthermore, such a click reaction allowed the localization of a bioactive compound inside living cells by fluorescence measurements. Chelating azides were designed to form clickable copper complexes for efficient ligation with alkynes in complex biological media. Among a series of azides that bear nitrogen heterocycles, a bis(triazole) azide allowed ultra-fast click reactions with alkynes within seconds under diluted conditions. The reactivity and stability of this copper complex enabled efficient click reactions inside living cells.

Thiophene-based compounds as fluorescent tags to study mesenchymal stem cell uptake and release of taxanes

Human mesenchymal stem cells (hMSC) are multipotent cells that display the unique ability to home and engraft in tumor stroma. This remarkable tumor tropic property has generated a great deal of interest in many clinical settings. Recently, we showed that hMSC represent an excellent base for cell-mediated anticancer therapy since they are able to internalize paclitaxel (PTX) and to release it in an amount sufficient to inhibit tumor cell proliferation. In order to shed light on the dynamics of drug uptake and release, in the present paper we describe the synthesis of two novel thiophene-based fluorophore-paclitaxel conjugates, namely PTX-F32 and PTX-F35, as tools for in vitro drug tracking. We aimed to study the ability of these novel derivatives to be efficiently internalized by hMSC and, in a properly engineered coculture assay, to be released in the medium and taken up by tumor cells. In order to ensure better stability of the conjugates toward enzymatic hydrolysis, the selected oligothiophenes were connected to the taxol core at the C7 position through a carbamate linkage between PTX and the diamino linker. Antiproliferative experiments on both tumor cells and stromal cells clearly indicate that, in good correlation with the parent compound, cells are sensitive to nanomolar concentrations of the fluorescent conjugates. Moreover, in the coculture assay we were able to monitor, by fluorescence microscopy, PTX-F32 trafficking from hMSC toward glioblastoma U87 tumor cells. Our work paves the way for novel possibilities to perform extensive and high quality fluorescence-based analysis in order to better understand the cellular mechanisms involved in drug trafficking, such as microvescicle/exosome mediated release, in hMSC vehicle cells.

CABAZITAXEL, RELATED COMPOUNDS AND METHODS OF SYNTHESIS

The invention provides new cabazitaxel isoserine ester intermediates and new synthetic methods, and a preparation method for the anti-tumour drugs cabazitaxel, docetaxel and paclitaxel from the new cabazitaxel isoserine intermediates.

Preparation of fluorescent tubulin binders

Thiocolchicine, taxol and cephalomannine have been used as building blocks for the preparation of four different fluorescent compounds designed to image the tubulin/microtubule network in cells. Thiocolchicine gave the best results and, in particular, the compound derived from conjugation with fluorescein minimally inhibits tubulin polymerization, is cell permeable and binds microtubules. Thus, it meets some of the demanding requirements for a new fluorescent dye that can secure a direct assay to evidence the tubulin/microtubules network in cells.

CABAZITAXEL, RELATED COMPOUNDS AND METHODS OF SYNTHESIS

The invention provides new cabazitaxel isoserine ester intermediates and new synthetic methods, and a preparation method for the anti-tumour drugs cabazitaxel, docetaxel and paclitaxel from the new cabazitaxel isoserine intermediates.

Chemo-enzymatic synthesis of ester-linked taxol-oligosaccharide conjugates as potential prodrugs

7-Glycolylpaclitaxel 2″-O-α-glucooligosaccharides, novel taxol (paclitaxel) prodrugs of ester-linked oligosaccharide series compounds, were synthesized by chemo-enzymatic procedures, including enzymatic transglycosylations with α-glucosidase and cyclodext

Synthesis of 7- and 10-spermine conjugates of paclitaxel and 10-deacetyl-paclitaxel as potential prodrugs

Efficient syntheses of two taxol analogs bearing the linear polyamine spermine at 7- and 10-positions of paclitaxel and 10-deacetyl-paclitaxel have been developed. These polyamine-taxol-conjugates were isolated as water soluble difluoride salts. The aim o