117527-51-2

Upstream product

• 108-55-4 glutaric anhydride, 
• 33069-62-4 taxol 

Downstream Products

• 1001441-14-0 paclitaxel-glutaric acid-N-hydroxysuccinimide 
• 1330703-36-0 C₆₁H₆₆F₂N₄O₂₀ 
• 915095-26-0 paclitaxel-2'-hemiglutarate 
• 117527-57-8 C₅₇H₆₉N₃O₁₆ 

Relevant academic research and scientific papers

Synthesis of congeners and prodrugs. 3. Water-soluble prodrugs of taxol with potent antitumor activity

Taxol has shown good in vivo antitumor activity in a number of test systems. The formulation of taxol for antitumor testing has been difficult. Esterification at either C-2' or C-7 resulted in loss of in vitro tubulin assembly activity but not cytotoxicit

Synthesis and antiproliferative activities of conjugates of paclitaxel and camptothecin with a cyclic cell-penetrating peptide

Cell-penetrating peptide [WR]5 has been previously shown to be an efficient molecular transporter for various hydrophilic and hydrophobic molecules. The peptide was synthesized using Fmoc/tBu solid-phase chemistry, and one arginine was replaced with one lysine to enable the conjugation with the anticancer drugs. Paclitaxel (PTX) was functionalized with an esterification reaction at the C20 hydroxyl group of PTX with glutaric anhydride and conjugated with the cyclic peptide [W(WR)4K(βAla)] in DMF to obtain the peptide-drug conjugate PTX1. Furthermore, camptothecin (CPT) was modified at the C(20)-hydroxyl group through the reaction with triphosgene. Then, it was conjugated with two functionalized cyclic peptides through a formyl linker affording two different conjugates, namely CPT1 and CPT2. All the conjugates showed better water solubility as compared to the parent drug. The cytotoxicity assay of the drugs and their conjugates with the peptides were evaluated in the human breast cancer MCF-7 cell line. PTX inhibited cell proliferation by 39% while the PTX-peptide conjugate inhibited the proliferation by ~18% after 72 h incubation. On the other hand, CPT, CPT1, and CPT2 reduced the cell proliferation by 68%, 39%, and 62%, respectively, in the MCF-7 cell lines at 5 μM concentration after 72 h incubation.

Paclitaxel weakly acidic derivative active medicine carrier liposome and preparation method and application thereof

The invention belongs to the field of liposome drug delivery, and relates to a paclitaxel weakly acidic derivative active medicine carrier liposome and a preparation method and application thereof. The paclitaxel weakly acidic derivative is provided, and

Simple weak-acid derivatives of paclitaxel for remote loading into liposomes and improved therapeutic effects

Liposomes are among the most successful nanocarriers; several products have been marketed, all of which were prepared by active loading methods. However, poorly water-soluble drugs without ionizable groups are usually incorporated into the lipid bi-layer

Taxane drug and doxorubicin prodrug self-assembled nanoparticles and application thereof

The invention belongs to the field of new auxiliary materials and new dosage forms of pharmaceutical preparations, relates to taxane drug and doxorubicin prodrug self-assembled nanoparticles and application thereof, and in particular relates to synthesis

RATIOMETRIC COMBINATORIAL DRUG DELIVERY

The present teachings include ratiometric combinatorial drug delivery including nanoparticles, multi-drug conjugates, pharmaceutical compositions, methods of producing such compositions and methods of using such compositions, including in the treatment of

Phospholipid Ether Analogs as Cancer-Targeting Drug Vehicles

The present invention is directed to therapeutic compounds capable of targeting cancer cells and cancer stem cells. The present invention is further directed to compositions comprising these therapeutic compounds and methods of treating cancer comprising

BIOLOGICAL MATERIALS AND USES THEREOF

The invention provides compounds comprising a therapeutic agent coupled to a carrier molecule, with a minimum coupling ratio of 5: 1; wherein the carrier molecule is (i) an antibody fragment or derivative thereof or (ii) an antibody mimetic or derivative thereof; and wherein the therapeutic agents are coupled onto a lysine amino acid residue; and further wherein the therapeutic agent is not a photosensitising agent. There is also provided uses, methods relating to such compounds, as well as processes for their manufacture.

Combinatorial drug conjugation enables nanoparticle dual-drug delivery

A new approach to loading multiple drugs onto the same drug-delivery nanocarrier in a precisely controllable manner, by covalently preconjugating multiple therapeutic agents through hydrolyzable linkers to form drug conjugates, is reported. In contrast to loading individual types of drugs separately, this drug-conjugates strategy enables the loading of multiple drugs onto the same carrier with a predefined stoichiometric ratio. The cleavable linkers allow the therapeutic activity of the individual drugs to be resumed after the drug conjugates are delivered into the target cells and unloaded from the delivery vehicle. As a proof of concept, the synthesis and characterization of paclitaxel-gemcitabine conjugates are demonstrated. The time-dependent hydrolysis kinetics and cytotoxicity of the combinatorial drug conjugates against human pancreatic cancer cells are examined. It is shown that the synthesized drug conjugates can be readily encapsulated into a lipid-coated polymeric drug-delivery nanoparticle, which significantly improves the cytotoxicity of the drug conjugates as compared to the free drug conjugates.

Synthesis of water-soluble dendrimers based on melamine bearing 16 paclitaxel groups

(Chemical Equation Presented) The design, synthesis, and characterization of triazine dendrimers derivatized with the anticancer agent paclitaxel are described. The precursor generation two dendrimer 1 is prepared in six linear steps in 64% overall yield