82333-93-5

Usage

Uses

Used in Chemical Synthesis:
1H-Pyrrole-1-hexanoyl chloride, 2,5-dihydro-2,5-dioxois used as a reagent in chemical synthesis for its unique properties and functional group. It can be employed in the preparation of various organic compounds, including pharmaceuticals, agrochemicals, and other specialty chemicals.
Used in Pharmaceutical Industry:
In the pharmaceutical industry, 1H-Pyrrole-1-hexanoyl chloride, 2,5-dihydro-2,5-dioxois used as a building block for the synthesis of drug candidates. Its unique structure and functional group can be utilized to create novel compounds with potential therapeutic applications.
Used in Agrochemical Industry:
1H-Pyrrole-1-hexanoyl chloride, 2,5-dihydro-2,5-dioxois also used in the agrochemical industry for the development of new pesticides and other crop protection agents. Its unique properties can contribute to the creation of more effective and environmentally friendly products.
Used in Specialty Chemicals:
In the specialty chemicals sector, 1H-Pyrrole-1-hexanoyl chloride, 2,5-dihydro-2,5-dioxois used as a key intermediate in the synthesis of various high-value compounds. Its unique structure and reactivity make it a valuable component in the development of advanced materials and other specialty products.

Upstream product

• 55750-53-3 2,5-Dihydro-2,5-dioxo-1H-pyrrole-1-hexanoic acid 

Downstream Products

• 1327231-54-8 6-(maleimido)-N-(2-(7-nitrobenzo[c][1,2,5]oxadiazol-4-ylamino)ethyl)hexanamide 
• 76-05-1 trifluoroacetic acid 

Relevant academic research and scientific papers

Chitosan-Based Peptidopolysaccharides as Cationic Antimicrobial Agents and Antibacterial Coatings

The rapid spread of multidrug-resistant bacteria has called for effective antimicrobial agents which work on a more direct mechanism of killing. Cationic peptidopolysaccharides are developed in the present work to mimic the peptidoglycan structure of bacteria and to enhance the membrane-compromising bactericidal efficacy. Antimicrobial CysHHC10 peptide was grafted to the C-2 (amino) or C-6 (hydroxyl) position of chitosan backbone via thiol-maleimide "click" conjugation, utilizing the maleimidohexanoic linkers. The peptidopolysaccharide with primary amino backbone intact (CSOHHC) exhibited higher bactericidal activity toward Gram-positive and Gram-negative bacteria, in comparison to that with amino backbone grafted with the peptide (CSNHHC). Both peptidopolysaccharides also exhibited lower hemolytic activity and cytotoxicity than free CysHHC10 peptide due to the moderation effect contributed by the chitosan backbone. For targeting the Gram-positive bacteria in particular, the CSOHHC expressed 4- and 2-fold increases in hemo- and cytoselectivity, respectively, as compared to the CysHHC10 peptide. In an extended application, peptidopolysaccharide antibacterial coatings were formed via layer-by-layer assembly with tannic acid. The peptidopolysaccharide coatings readily killed the adhered bacteria upon contact while being cytocompatible by maintaining more than 60% viability for the adhered fibroblasts. Therefore, the peptidoglycan-mimetic peptidopolysaccharides are potential candidates for anti-infective drugs in biomedical applications.

Clustered nanobody-drug conjugates for targeted cancer therapy

A clustered Nb-drug conjugate (cNDC?PEG) was designed using anti-EGFR Nb to specifically deliver Pt(iv) prodrugs to tumors. cNDC?PEG efficiently targets EGFR positive tumor cells, and the clustered cNDC?PEG is more efficient in inhibiting tumor growth in vivo than the monomeric NDC. This work provides a novel strategy for the construction of a multi-valent NDC using dendrimers. This journal is

Reversible crosslinking of lignin via the furan-maleimide Diels-Alder reaction

Two distinct functionalization schemes for Kraft lignin (KL) were developed to selectively incorporate furan and/or maleimide motifs as chain ends. The incorporation of furan functionalities was carried out by the selective and quantitative reaction of the lignin's phenolic OH groups with furfuryl glycidyl ether (FGE). Maleimide groups were introduced by esterifying the lignin's aliphatic and phenolic OH groups with 6 maleimidohexanoic acid (6-MHA), offering a high loading despite a somewhat incomplete conversion. Furan- and maleimide-functionalized lignins were subsequently combined to generate crosslinking via the Diels-Alder (DA) [4 + 2] cycloaddition reaction. The formation of the DA adduct was confirmed by 1H NMR. Under appropriate conditions, the formation of a gel was apparent, which turned back into the liquid state after performing the corresponding retro-DA reaction upon heating to 120 °C. This study reveals the significant versatility and potential of the developed strategy for the utilization of lignin-based recyclable networks.

Honokiol Prodrug Nanoparticles Based on in Situ Albumin Binding for Long Circulation and High Tumor Uptake

Honokiol (HK) has antiproliferation effects against numerous cancer cells, but its low solubility and bioavailability impede its application. In this study, a prodrug of HK (HP) featuring a maleimide group was synthesized and then mixed with tocopherol polyethylene glycol succinate to prepare prodrug nanoparticles (HP-NPs). In vitro albumin binding experiments showed that HP rapidly reacted with the cysteine thiols of albumin to form a covalent conjugate that released HK slowly in the LLC tumor cell line. In vitro cell apoptosis and uptake assays showed that the cellular uptake of the HK increased into the LLC cells as the albumin concentration increased. Strikingly, in vivo pharmacokinetics and pharmacodynamics measurements demonstrated that the HP-NPs significantly prolonged the circulation and increased tumor accumulation. Taken together, our study demonstrated, both in vitro and in vivo, that the albumin-based HP-NPs delivery system holds significant potential toward the treatment of lung cancer in clinical studies.

ANTIBODY DRUG CONJUGATES OF KINESIN SPINDEL PROTEIN (KSP) INHIBITORS WITH ANTIB7H3-ANTIBODIES

The present application relates to novel binder drug conjugates (ADCs), to active metabolites of these ADCs, to processes for preparing these ADCs, to the use of these ADCs for the treatment and/or prophylaxis of diseases and to the use of these ADCs for preparing medicaments for treatment and/or prophylaxis of diseases, in particular hyperproliferative and/or angiogenic disorders such as, for example, cancer diseases. Such treatments can be effected as monotherapy or else in combination with other medicaments or further therapeutic measures.

Photopolymerization of maleimide perfluoropolyalkylethers without a photoinitiator

Perfluoropolyalkylethers derived from hexafluoropropylene oxide were functionalized with maleimide groups. Irradiated by UV-light, the new maleimide macromonomers demonstrated very fast polymerization kinetics with a curing time as fast as 8 s. The effect on photopolymerization of different features such as the molecular weight of the fluorinated chain and the chain length of the hydrogenated spacer were studied, as well as the influence of the type of photoinitiator and the presence of air. Thermal and surface properties of the UV-cured polymers were examined and were typical to fluoropolymers in view of water–oil repellent coatings.

DELIVERY SYSTEMS FOR CONTROLLED DRUG RELEASE

The present invention provides a compound having the structure of Formula (I) or a pharmaceutically acceptable salt, hydrate, solvate, or isomer thereof, for the controlled delivery and release of Agent.

MAYTANSINOID-BASED DRUG DELIVERY SYSTEMS

The present subject matter provides for albumin-binding prodrugs, maytansinoid-based compounds, and uses thereof.

ALBUMIN-BINDING PRODRUGS OF AURISTATIN E DERIVATIVES

The present disclosure provides for albumin-binding prodrugs of auristatin E derivatives and uses thereof.

Synthesis and anti-cancer evaluation of folic acid-peptide- paclitaxel conjugates for addressing drug resistance

The drug resistance and the poor water solubility are major limitations of paclitaxel (PTX) of based chemotherapy. To conquer the two problems, targeting folate (FA) receptor PTX-lytic peptides conjugates were synthesized and evaluated. Compared with PTX, FA-P3-PTX and FA-P7-PTX displayed significantly enhanced cell toxicity in many cancer cells, particularly drug resistant cancer cells MCF-7/PTX. FA-P7-PTX possessed stronger effect on cell toxicity (IC50 = 2.92 ± 0.2 μM), membrane disrupting activity and pro-apoptosis in MCF-7/PTX cells than FA-P3-PTX. Further investigation displayed that the anti-cancer mechanisms of FA-P3-PTX and FA-P7-PTX might be a mitochondrial impairment and caspase-3-dependent apoptotic cell death. Furthermore, the in vivo antitumor efficacy study confirmed that FA-P7-PTX performed more stronger potency in inhibition of tumors growth than PTX. The study demonstrated that conjugate FA-P7-PTX with superior properties for antineoplastic activity, which makes it a promising potential candidate for drug-resistant cancer therapy.