Category: 42074-68-0

Stevenson, Graeme I. published the artcileSolid-phase synthesis of Biotin-S-Farnesyl-L-Cysteine, a surrogate substrate for isoprenylcysteine Carboxylmethyltransferase (ICMT), SDS of cas: 42074-68-0, the publication is Bioorganic & Medicinal Chemistry Letters (2013), 23(20), 5671-5673, database is CAplus and MEDLINE.

Inhibition of isoprenylcysteine carboxylmethyltransferase (ICMT) is of particular interest as a potential target for the development of cancer chemotherapeutic agents. Screening for inhibitors of ICMT utilizes a scintillation proximity assay (SPA) in which biotin-S-farnesyl-L-cysteine (BFC) acts as a surrogate substrate. A solid-phase synthesis protocol for the preparation of BFC using 2-chlorotrityl chloride resin as a solid support has been developed to provide sufficient supply of BFC for high throughput screening (HTS) and subsequent chem. campaigns to target inhibitors of ICMT. The BFC prepared by this method can be produced quickly on large scale and is stable when stored at -20° as a solid, in solution, or on the resin.

Bioorganic & Medicinal Chemistry Letters published new progress about 42074-68-0. 42074-68-0 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Benzyl chloride,Benzene, name is 2-Chlorotrityl chloride, and the molecular formula is C7H13NO2, SDS of cas: 42074-68-0.

Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics

Liang, Chunhui published the artcileEnhanced cellular uptake and nuclear accumulation of drug-peptide nanomedicines prepared by enzyme-instructed self-assembly, Formula: C19H14Cl2, the publication is Journal of Controlled Release (2020), 109-117, database is CAplus and MEDLINE.

Subcellular delivery of nanomedicines has emerged as a promising approach to enhance the therapeutic efficacy of anticancer drugs. Nuclear accumulation of anticancer drugs are essential for its therapeutic efficacy because their targets are generally located within the nucleus. However, strategies for the nuclear accumulation of nanomedicines with anticancer drugs rarely reported. In this study, we reported a promising nanomedicine, comprising a drug-peptide amphiphile, with enhanced cellular uptake and nuclear accumulation capability for cancer therapy. The drug-peptide amphiphile consisted of the peptide ligand PMI (TSFAEYWNLLSP), which was capable of activating the p53 gene by binding with the MDM2 and MDMX located in the cell nucleus. Peptide conformations could be finely tuned by using different strategies including heating-cooling and enzyme-instructed self-assembly (EISA) to trigger mol. self-assembly at different temperatures Due to the different peptide conformations, the drug-peptide amphiphile self-assembled into nanomedicines with various properties, including stabilities, cellular uptake, and nuclear accumulation. The optimized nanomedicine formed by EISA strategy at a low temperature of 4 C showed enhanced cellular uptake and nuclear accumulation capability, and thus exhibited superior anticancer ability both in vitro and in vivo. Overall, our study provides a useful strategy for finely tuning the properties and activities of peptide-based supramol. nanomaterials, which may lead to optimized nanomedicines with enhanced performance.

Journal of Controlled Release published new progress about 42074-68-0. 42074-68-0 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Benzyl chloride,Benzene, name is 2-Chlorotrityl chloride, and the molecular formula is C19H14Cl2, Formula: C19H14Cl2.

Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics

Feng, Ke published the artcileModular Design of Poly(norbornenes) for Organelle-Specific Imaging in Tumor Cells, COA of Formula: C19H14Cl2, the publication is Biomacromolecules (2016), 17(2), 538-545, database is CAplus and MEDLINE.

Through modular ROMP (ring-opening metathesis polymerization) directly from monomeric norbornenes of bioactive peptides, rhodamine B chromophore, and PEG solubilizer, we designed and synthesized a series of water-soluble poly(norbornenes) with organelle-specific imaging capability in tumor cells. For the selection of F_xrF_xK, TAT, and SV40 peptide sequences, these fluorescence probes exhibited different targeting specificity toward mitochondria, lysosome, and nucleolus, resp., based on the same poly(norbornene) backbonds. More importantly, the ROMP strategy enables selective combination from various monomers and allows programmable biofunctionalization via peptide sequence permutations, which would greatly extend the biomedical applications such as imaging, diagnosis, and therapy for these synthetic polymers.

Biomacromolecules published new progress about 42074-68-0. 42074-68-0 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Benzyl chloride,Benzene, name is 2-Chlorotrityl chloride, and the molecular formula is C19H14Cl2, COA of Formula: C19H14Cl2.

Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics

Liu, Chenguang published the artcileAutomated synthesis of prexasertib and derivatives enabled by continuous-flow solid-phase synthesis, Recommanded Product: 2-Chlorotrityl chloride, the publication is Nature Chemistry (2021), 13(5), 451-457, database is CAplus and MEDLINE.

Recent advances in end-to-end continuous-flow synthesis are rapidly expanding the capabilities of automated customized syntheses of small-mol. pharmacophores, resulting in considerable industrial and societal impacts; however, many hurdles persist that limit the number of sequential steps that can be achieved in such systems, including solvent and reagent incompatibility between individual steps, cumulated byproduct formation, risk of clogging and mismatch of timescales between steps in a processing chain. To address these limitations, herein a strategy that merges solid-phase synthesis and continuous-flow operation, enabling push-button automated multistep syntheses of active pharmaceutical ingredients, is reported. The application of this methodol. is demonstrated with a six-step synthesis of prexasertib in 65% isolated yield after 32 h of continuous execution. As there are no interactions between individual synthetic steps in the sequence, the established chem. recipe file was directly adopted or slightly modified for the synthesis of twenty-three prexasertib derivatives, enabling both automated early and late-stage diversification.

Nature Chemistry published new progress about 42074-68-0. 42074-68-0 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Benzyl chloride,Benzene, name is 2-Chlorotrityl chloride, and the molecular formula is C19H14Cl2, Recommanded Product: 2-Chlorotrityl chloride.

Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics

Zhang, Jing published the artcileMultifunctional Mesoporous Silica Nanoparticles Based on Charge-Reversal Plug-Gate Nanovalves and Acid-Decomposable ZnO Quantum Dots for Intracellular Drug Delivery, Application of 2-Chlorotrityl chloride, the publication is ACS Applied Materials & Interfaces (2015), 7(48), 26666-26673, database is CAplus and MEDLINE.

A novel type of pH-responsive multifunctional mesoporous silica nanoparticle (MSN) was developed for cancerous cells drug delivery and synergistic therapy of tumor. MSNs were covered with a kind of cell-penetrating peptide, deca-lysine sequence (K₁₀), to enhance their escape from the endosomes. After K₁₀‘s primary amines were reacted with citraconic anhydride to form acid-labile β-carboxylic amides, zinc oxide (ZnO) quantum dots (QDs) were introduced to cap MSNs via electrostatic interaction. The obtained ZnO@MSN drug-delivery system (DDS) achieves “zero-premature” drug release under a physiol. environment. However, once the DDS is transferred to the cancerous cells’ acidic endosome, ZnO QDs would rapidly dissolve and the acid-labile amides on the side chain of K₁₀ would hydrolyze to regenerate primary amines, resulting in the uncapping of MSNs and exposure of the cell-penetrating peptide K₁₀. The regenerated K₁₀ could help the DDS escape from the endosome and efficiently release the loaded drugs inside the cells. At the meantime, because of the cytotoxicity of ZnO QDs at their destination, the ZnO@MSN DDS may achieve a synergistic antitumor effect to improve the therapeutic index.

ACS Applied Materials & Interfaces published new progress about 42074-68-0. 42074-68-0 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Benzyl chloride,Benzene, name is 2-Chlorotrityl chloride, and the molecular formula is C4H6O3, Application of 2-Chlorotrityl chloride.

Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics

Androvic, Ladislav published the artcileCyclotriphosphazene-Based Star Copolymers as Structurally Tunable Nanocarriers with Programmable Biodegradability, COA of Formula: C19H14Cl2, the publication is Macromolecules (Washington, DC, United States) (2021), 54(7), 3139-3157, database is CAplus.

Myriad nanocarriers have been developed to improve the therapeutic index of low-mol.-weight drugs for cancer treatment, but many have suboptimal size and/or are too stable for optimal penetration into tumors and their subsequent excretion from the body. To address this challenge, we developed a series of novel nanocarriers based on star polymers consisting of hydrophilic poly[N-(2-hydroxypropyl)methacrylamide] (PHPMA) or poly(ethylene glycol) (PEG) polymer arms attached to hexavalent cyclotriphosphazene (CTP)-derived cores through either stable or stimuli-responsive linkers. The star polymers were assembled using either “grafting from” or “grafting onto” approaches and characterized by quant. arm substitution at the core. The resulting star polymers were precisely defined water-soluble nanomaterials with a suitable hydrodynamic size (~10-25 nm) for tumor uptake; those with stimuli-responsive linkers exhibited programmable pH- or cathepsin-mediated degradability. Finally, low-mol.-weight drugs-an anthracycline-based cancerostatic and an imidazoquinoline-based immunostimulant-were linked to exemplary CTP-based star polymers to demonstrate their suitability for drug delivery.

Macromolecules (Washington, DC, United States) published new progress about 42074-68-0. 42074-68-0 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Benzyl chloride,Benzene, name is 2-Chlorotrityl chloride, and the molecular formula is C19H14Cl2, COA of Formula: C19H14Cl2.

Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics

Kulkarni, Sameer S. published the artcileDiselenide-selenoester ligation for chemical protein synthesis, COA of Formula: C19H14Cl2, the publication is Nature Protocols (2019), 14(7), 2229-2257, database is CAplus and MEDLINE.

Chemoselective peptide ligation methods have provided synthetic access to numerous proteins, including those bearing native post-translational modifications and unnatural labels. This protocol outlines the chem. synthesis of proteins using a recently discovered reaction (diselenide-selenoester ligation (DSL)) in a rapid, additive-free manner. After ligation, the products can be chemoselectively deselenized to produce native peptide and protein products. We describe methods for the synthesis of suitably functionalized peptide diselenide and peptide selenoester fragments via Fmoc-solid-phase peptide synthesis (SPPS) protocols, fusion of these fragments by DSL, and the chemoselective deselenization of the ligation products to generate native synthetic proteins. We demonstrate the method’s utility through the total chem. synthesis of the post-translationally modified collagenous domain of the hormone adiponectin via DSL-deselenization at selenocystine (the oxidized form of selenocysteine) and the rapid preparation of two tick-derived thrombin-inhibiting proteins by DSL-deselenization at β-selenoaspartate and γ-selenoglutamate. This method should find widespread use for the rapid synthesis of proteins, including cases in which other peptide ligation methods cannot be used (or cannot be used efficiently), e.g., at sterically hindered or deactivated acyl donors. The method’s speed and efficiency may render it useful in the generation of synthetic protein libraries. Each protein discussed can be synthesized within 15 working days from resin loading and can be readily produced by practitioners with master’s-level experience in organic chem. Each synthesis using these protocols was performed independently by two labs (one academic and one industrial), which attained comparable yields of the protein products.

Nature Protocols published new progress about 42074-68-0. 42074-68-0 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Benzyl chloride,Benzene, name is 2-Chlorotrityl chloride, and the molecular formula is C19H14Cl2, COA of Formula: C19H14Cl2.

Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics

Hu, Yuhan published the artcileEnzyme-instructed self-assembly of peptide-drug conjugates in tear fluids for ocular drug delivery, Recommanded Product: 2-Chlorotrityl chloride, the publication is Journal of Controlled Release (2022), 261-271, database is CAplus and MEDLINE.

In vivo self-assembly of small mols. offers an excellent opportunity for targeted and long-term accumulation of a therapeutic agent at the lesion site. Here we demonstrate the strategy of enzyme-instructed self-assembly (EISA) by designing a phosphorylated peptide-drug (IBF-HYD-GFFpY) precursor through the ester bond to release active drugs at the target site. Meanwhile, the in vivo assembly can be achieved by the catalysis of alk. phosphatase (ALP) in the tear fluid for ocular drug delivery efficiently. The in vitro enzymic experiments indicate that the dephosphorylation of IBF-HYD-GFFpY occurs firstly with the yield of IBF-HYD-GFFY which subsequently self-assembles into the supramol. hydrogel to afford sustained drug release over 96 h. In the treatment of lipopolysaccharide (LPS)-activated Raw 264.7 macrophages, IBF-HYD-GFFpY exerts the more potent anti-inflammatory efficacy than that of free ibuprofen (IBF) at the concentration of 200 μM. Moreover, the aqueous solution of IBF-HYD-GFFpY via topical instillation hardly causes ocular irritation, and displays longer precorneal retention compared to the conventional eye drop formulation. In addition, in the in vivo study, a rabbit model of endotoxin-induced uveitis (EIU) evidences the comparable therapeutic efficacy of IBF-HYD-GFFpY eye drops with that of clin. used 0.1 wt% diclofenac (DIC) sodium eye drops by the reduction of macrophage and leukocyte influx. This work, in situ EISA in the tear microenvironment directing in vivo self-assembly of small mols., may guide a powerful approach for developing enzymic self-assembled mols. as an efficient delivery system of ocular drugs.

Journal of Controlled Release published new progress about 42074-68-0. 42074-68-0 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Benzyl chloride,Benzene, name is 2-Chlorotrityl chloride, and the molecular formula is C19H14Cl2, Recommanded Product: 2-Chlorotrityl chloride.

Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics

Li, Xincan published the artcileEffects of cyclization on activity and stability of α-conotoxin TxIB, COA of Formula: C19H14Cl2, the publication is Marine Drugs (2020), 18(4), 180, database is CAplus and MEDLINE.

A α-Conotoxin TxIB specifically blocked α6/α3β2β3 acetylcholine receptors (nAChRs), and it could be a potential probe for studying addiction and other diseases related to α6/α3β2β3 nAChRs. However, as a peptide, TxIB may suffer from low stability, short half-life, and poor bioavailability. In this study, cyclization of TxIB was used to improve its stability. Four cyclic mutants of TxIB (cTxIB) were synthesized, and the inhibition of these analogs on α6/α3β2β3 nAChRs as well as their stability in human serum were measured. All cyclized analogs had similar activity compared to wild-type TxIB, which indicated that backbone cyclization of TxIB had no significant effect on its activity. Cyclization of TxIB with a seven-residue linker improved its stability significantly in human serum. Besides this, the results showed that cyclization maintained the activity of α-conotoxin TxIB, which is conducive to its future application.

Marine Drugs published new progress about 42074-68-0. 42074-68-0 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Benzyl chloride,Benzene, name is 2-Chlorotrityl chloride, and the molecular formula is C19H14Cl2, COA of Formula: C19H14Cl2.

Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics

Seibold, Uwe published the artcileRational Design, Development, and Stability Assessment of a Macrocyclic Four-Hydroxamate-Bearing Bifunctional Chelating Agent for ⁸⁹Zr, Product Details of C19H14Cl2, the publication is ChemMedChem (2017), 12(18), 1555-1571, database is CAplus and MEDLINE.

Zirconium-89 is a positron-emitting radionuclide of high interest for medical imaging applications with positron emission tomog. (PET). For the introduction of this radiometal into biol. active targeting vectors, the chelating agent desferrioxamine B (DFO) is commonly applied. However, DFO is known to form ⁸⁹Zr complexes of limited in vivo stability. Herein we describe the rational design and chem. development of a new macrocyclic four-hydroxamate-bearing chelating agent-1,10,19,28-tetrahydroxy-1,5,10,14,19,23,28,32-octaazacyclohexatriacontan-2,6,11,15,20,24,29,33-octaone (CTH36)-for the stable complexation of Zr⁴⁺. For this purpose, we first performed computational studies to determine the optimal chelator geometry before we developed different synthesis pathways toward the target structures. The best results were obtained using an efficient solution-phase-based synthesis strategy toward the target chelating agent. To enable efficient and chemoselective conjugation to biomols., a tetrazine-modified variant of CTH36 was also developed. The excellent conjugation characteristics of the so-functionalized chelator were demonstrated on the example of the model peptide TCO-c(RGDfK). We determined the optimal ⁸⁹Zr radiolabeling parameters for CTH36 as well as its bioconjugate, and found that ⁸⁹Zr radiolabeling proceeds efficiently under very mild reaction conditions. Finally, we performed comparative complex stability tests for ⁸⁹Zr-CHT36-c(RGDfK) and ⁸⁹Zr-DFO-c(RGDfK), showing improved complex stability for the newly developed chelator CTH36.

ChemMedChem published new progress about 42074-68-0. 42074-68-0 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Benzyl chloride,Benzene, name is 2-Chlorotrityl chloride, and the molecular formula is C8H7NO4, Product Details of C19H14Cl2.

Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics