114655-02-6Relevant articles and documents
Paclitaxel prodrugs with sustained release and high solubility in poly(ethylene glycol)-b-poly(ε-caprolactone) micelle nanocarriers: Pharmacokinetic disposition, tolerability, and cytotoxicity
Forrest, M. Laird,Yanez, Jaime A.,Remsberg, Connie M.,Ohgami, Yusuke,Kwon, Glen S.,Davies, Neal M.
, p. 194 - 206 (2008)
Purpose. Develop a Cremophor and solvent free formulation of paclitaxel using amphiphilic block co-polymer micelles of poly(ethylene glycol)-b-poly(ε-caprolactone) (PEG-b-PCL) and characterize their release, solubility, cytotoxicity, tolerability, and dis
Synthesis of a Fluorescent Analogue of Paclitaxel That Selectively Binds Microtubules and Sensitively Detects Efflux by P-Glycoprotein
Lee, Molly M.,Gao, Zhe,Peterson, Blake R.
, p. 6927 - 6931 (2017)
The anticancer drug paclitaxel (Taxol) exhibits paradoxical and poorly understood effects against slow-growing tumors. To investigate its biological activity, fluorophores such as Oregon Green have been linked to this drug. However, this modification incr
Paclitaxel-functionalized gold nanoparticles
Gibson, Jacob D.,Khanal, Bishnu P.,Zubarev, Eugene R.
, p. 11653 - 11661 (2007)
Here we describe the first example of 2 nm gold nanoparticles (Au NPs) covalently functionalized with a chemotherapeutic drug, paclitaxel. The synthetic strategy involves the attachment of a flexible hexaethylene glycol linker at the C-7 position of pacli
A paclitaxel prodrug with bifunctional folate and albumin binding moieties for both passive and active targeted cancer therapy
Shan, Lingling,Zhuo, Xin,Zhang, Fuwu,Dai, Yunlu,Zhu, Guizhi,Yung, Bryant C.,Fan, Wenpei,Zhai, Kefeng,Jacobson, Orit,Kiesewetter, Dale O.,Ma, Ying,Gao, Guizhen,Chen, Xiaoyuan
, p. 2018 - 2030 (2018)
Folate receptor (FR) has proven to be a valuable target for chemotherapy using folic acid (FA) conjugates. However, FA-conjugated chemotherapeutics still have low therapeutic efficacy accompanied with side effects, resulting from complications such as sho
Ferrocenyl Paclitaxel and Docetaxel Derivatives: Impact of an Organometallic Moiety on the Mode of Action of Taxanes
Wieczorek, Anna,B?au?, Andrzej,?al, Aleksandra,Arabshahi, Homayon John,Reynisson, Jóhannes,Hartinger, Christian G.,Rychlik, B?a?ej,Pla?uk, Damian
, p. 11413 - 11421 (2016)
A series of ferrocenyl analogues and derivatives of paclitaxel and docetaxel were synthesised and assayed for their antiproliferative/cytotoxic effects, impact on the cell cycle distribution and ability to induce tubulin polymerisation. The replacement of the 3′-N-benzoyl group of paclitaxel with a ferrocenoyl moiety, in particular, led to formation of an analogue that was at least one order of magnitude more potent in terms of antiproliferative activity than the parent compound (IC50values of 0.11 versus 1.11 μm, respectively), but still preserved the classical taxane mode of action, that is, microtubule stabilisation leading to mitotic arrest. Molecular docking studies revealed an unexpected binding pocket in the tubulin structure for the ferrocenoyl group introduced in the paclitaxel backbone.
The effect of drug position on the properties of paclitaxel-conjugated gold nanoparticles for liver tumor treatment
Wang, Huaisong,Wang, Lin,Gao, Yueyuan,Ding, Ya
, p. 1041 - 1045 (2021)
Structure-efficacy effect of small molecular drug attracts wide attentions, but it has always been ignored in nanomedicine research. To reveal the efficacy modulation of nanomedicine, we developed a new type of paclitaxel (PTX)-conjugated gold nanoparticl
Synthesis and Biological Investigation of Bile Acid-Paclitaxel Hybrids
Casciano, Fabio,Marchesi, Elena,Melloni, Elisabetta,Navacchia, Maria Luisa,Perrone, Daniela,Preti, Lorenzo,Rimondi, Erika,Romani, Arianna,Secchiero, Paola
, (2022/01/20)
Chenodeoxycholic acid and ursodeoxycholic acid (CDCA and UDCA, respectively) have been conjugated with paclitaxel (PTX) anticancer drugs through a high-yield condensation reaction. Bile acid-PTX hybrids (BA-PTX) have been investigated for their pro-apopto
Disulfide-crosslinked reduction-responsive Prodrug Micelles for On-demand Paclitaxel Release
Wang, Zhi,Ling, Longbing,Xia, Qing,Li, Xinsong
, (2019/08/01)
In this report, disulfide-crosslinked paclitaxel (PTX) prodrug micelles were developed through covalently conjugating PTX onto water soluble poly(ethylene glycol)-dihydrolipoic acid (MeO-PEG2k-DHLA) via a disulfide linkage and studied their perspectives for chemotherapic antitumor capacity. The polymer-PTX prodrug (MeO-PEG2k-SS-PTX), structurally determined by 1H NMR, possessed high PTX content up to 26 wt% and exhibited sharp reduction-responsive behavior. MeO-PEG2k-SS-PTX micelles were then subjected to crosslinking by oxidization of thiol (-SH) groups in the core of micellar particles after self-assembly of the amphimictic prodrug. The resultant crosslinked micelles were stable with spherical morphology having the uniform size of 87.67 nm in phosphate buffer (PBS, pH 7.4), as confirmed by transmission electron microscope (TEM) and dynamic light scattering (DLS). The cross-linked micelles based on the redox-sensitive MeO-PEG2k-SS-PTX prodrug exhibited an obvious glutathione (GSH)-dependant manner of fast PTX release with appropriate 65.6% in 12 h and 92.6% in 72 h after incubation in PBS medium containing 10 mM GSH. MTT assay together with apoptosis analysis showed that cross-linked MeO-PEG2k-SS-PTX micelles worked the higher antitumor activity against MCF-7, A549, BEL-7402 and 4T1 cells, using free PTX as a positive control. More importantly, such micelles were found to hold a longer circulation time in bloodstream and be able to passively targeting accumulate in tumor sites of 4T1-transplanted BALB/c mice model.
Taxol-DHA-dextran coupling polymer, synthetic method thereof and application of polymer
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Paragraph 0060; 0139; 0154-0156, (2019/10/01)
The invention provides a taxol-DHA-dextran coupling polymer, a synthetic method thereof and an application of the polymer, and belongs to the technical field of biological medicines. According to thepolymer, polysaccharides serve as polymer drug-loaded frameworks, so that an anti-tumor drug-polysaccharide passive targeted coupling polymer is prepared, taxol can be passively targeted into a tumortissue by the aid of an EPR effect, and an anti-tumor function is played. Water solubility and biocompatibility of taxol medicines can be increased, accumulation of anti-tumor medicines in the tumor tissue can be increased under the passive targeted action, general side effect and nervous side effect of the taxol medicines are reduced, and the polymer has good practical application values.
Synthesis and biological evaluation of PSMA-targeting paclitaxel conjugates
Machulkin, Alexey E.,Skvortsov, Dmitry A.,Ivanenkov,Ber, Anton P.,Kavalchuk, Mikhail V.,Aladinskaya, Anastasia V.,Uspenskaya, Anastasia A.,Shafikov, Radik R.,Plotnikova, Ekaterina A.,Yakubovskaya, Raisa I.,Nimenko, Ekaterina A.,Zyk, Nikolay U.,Beloglazkina, Elena K.,Zyk, Nikolay V.,Koteliansky, Victor E,Majouga, Alexander G.
, p. 2229 - 2235 (2019/06/27)
Prostate cancer (PC) is the second most commonly occurring cancer in men. Conventional chemotherapy has wide variety of disadvantages such as high systemic toxicity and low selectivity. Targeted drug delivery is a promising approach to decrease side effec
