544429-89-2

Upstream product

• 59-30-3 folic acid 
• 6066-82-6 1-hydroxy-pyrrolidine-2,5-dione 
• 59-30-3 folate 

Relevant academic research and scientific papers

A step-wise synthetic approach is necessary to access γ-conjugates of folate: Folate-conjugated prodigiosenes

Despite the vast literature that describes reacting folic acid with a pharmacophore, this route is ineffective in providing the correct regioisomer of the resulting conjugate. We herein present a step-wise route to the preparation of nine folate conjugate

Ultrafast synthesis of stabilized gold nanoparticles using aqueous fruit extract of Limonia acidissima L. and conjugated epirubicin: Targeted drug delivery for treatment of breast cancer

In this study, a green chemistry approach was used for the quick synthesis (within 30 seconds) of gold nanoparticles (AuNPs) by using the fruit extract of Limonia acidissima L. The study focused on the formation of L. acidissima L. stabilized AuNPs withou

A with the folic acid receptor target combination of folic acid dimer compound and use thereof

The invention belongs to the medical field and discloses folic acid dimer compound combined with folate receptor targeting and an application thereof. The compound is X2-Y-Z-A, wherein X2 is lysine and folic acid connecting dimer or lysine and folic acid

TARGETING MICROBUBBLES

This invention related to manufactured microbubbles, as well as methods of using manufactured microbubbles, for example, in medicinal applications. The invention pertains to the physical structure and materials of the microbubbles, as well as to methods for manufacturing microbubbles, methods for targeting microbubbles for specific medicinal applications, and methods for delivering microbubbles in medical treatment.

Folate-cyclodextrin conjugates as carriers of the platinum(IV) complex LA-12

Folic acid has emerged as an interesting cell-targeting moiety and a number of drugs have been conjugated to folate. In this context, new conjugates of β-cyclodextrins with folate have been synthesised as drug carriers to improve their selectivity for cells overexpressing the folic acid receptor. In particular, both 3- and 6-functionalised β-cyclodextrins, linked to the α- or γ-carboxylic group of folic acid, have been synthesised and fully characterised. As a proof of concept, the antitumour platinum(IV) complex cis-trans-cis-[PtCl2(CH3CO2)2(adamantylamine)(NH3)] (LA-12) has been used as a guest drug. The LA-12-cyclodextrin inclusion complexes have been tested on tumour cells. In the presence of cyclodextrin-folate conjugates, LA-12 exhibited IC50 values four times smaller than those of LA-12 alone in MDA-MB-231 cells, which overexpress folic acid receptors on their membrane. No improvement of LA-12 cytotoxicity was found in control tumour cells that do not overexpress the folate receptor. Thus, the non-covalent approach, based on inclusion complexes with functionalised cyclodextrins, looks very promising for drug targeting. Drugs included: The antitumor drug cis-trans-cis-[PtCl2(CH3CO2)2(adamantlyamine)(NH3)] (LA-12) co-administered with 3- or 6-functionalised β-cyclodextrin conjugated with γ-folate (βCyD3-FAγ or βCyD6-FAγ) as an inclusion complex showed IC50 values significantly lower than that of LA-12 alone or LA-12 co-administered with βCyD in folate receptor-overexpressing cancer cells (see figure).

Multifunctional DNA-gold nanoparticles for targeted doxorubicin delivery

In this report we describe the synthesis, characterization, and cytotoxic properties of DNA-capped gold nanoparticles having attached folic acid (FA), a thermoresponsive polymer (p), and/or poly(ethylene glycol) (PEG) oligomers that could be used to deliver the anticancer drug doxorubicin (DOX) in chemotherapy. The FA-DNA oligomer used in the construction of the delivery vehicle was synthesized through the reaction of the isolated folic acid N-hydroxysuccinimide ester with the amino-DNA and the conjugated DNA product was purified using high performance liquid chromatography (HPLC). This approach ultimately allowed control of the amount of FA attached to the surface of the delivery vehicle. Cytotoxicity studies using SK-N-SH neuroblastoma cells with drug loaded delivery vehicles were carried out using a variety of exposure times (1-48 h) and recovery times (1-72 h), and in order to access the effects of varying amounts of attached FA, in culture media deficient in FA. DOX loaded delivery vehicles having 50% of the DNA strands with attached FA were more cytotoxic than when all of the strands contained FA. Since FA stimulates cell growth, the reduced cytotoxicity of vehicles fully covered with FA suggests that the stimulatory effects of FA can more than compensate for the cytotoxic effects of the drug on the cell population. While attachment of hexa-ethylene glycol PEG(18) to the surface of the delivery vehicle had no effect on cytotoxicity, 100% FA plus the thermoresponsive polymer resulted in IC50 = 0.48 ± 0.01 for an exposure time of 24 h and a recovery time of 1 h, which is an order of magnitude more cytotoxic than free DOX. Confocal microscopic studies using fluorescence detection showed that SK-N-SH neuroblastoma cells exposed to DOX-loaded vehicles have drug accumulation inside the cell and, in the case of vehicles with attached FA and thermoresponsive polymer, the drug appears more concentrated. Since the biological target of DOX is DNA, the latter observation is consistent with the high cytotoxicity of vehicles having both FA and the thermoresponsive polymer. The study highlights the potential of DNA-capped gold nanoparticles as delivery vehicles for doxorubicin in cancer chemotherapy.

LIPOPROTEIN NANOPLATFORMS

The present invention provides a non-naturally occurring lipoprotein nanoplatform ("LBNP") comprising at least one cell surface receptor ligand; at least one lipoprotein; and at least one diagnostic agent and/or at least one therapeutic agent. In embodime