Category: 42074-68-0

Kiran, Sonia published the artcileAlkaline phosphatase-triggered assembly of etoposide enhances its anticancer effect, Recommanded Product: 2-Chlorotrityl chloride, the publication is Chemical Communications (Cambridge, United Kingdom) (2018), 54(15), 1853-1856, database is CAplus and MEDLINE.

Etoposide is a cancer-targeting drug but an overdose of etoposide leads to immunosuppression in patients. Therefore, the development of a new strategy to enhance its anticancer effect, while in the meantime alleviating its adverse effects, is important but challenging. In this work, with the assistance of a hydrogelator precursor Nap-Phe-Phe-Tyr(H₂PO₃)-OH (1P), etoposide phosphate (EP) was subjected to alk. phosphatase (ALP)-triggered assembly, which obviously enhanced its anticancer efficacy in vitro and in vivo. In vitro tests indicated that the assembly of EP with 1P resulted in a slow release of etoposide and long-term inhibitory effects on HeLa cells. In vivo experiments indicated that, compared with those of EP-treated mice, the tumor growth of EP + 1P-treated mice was further inhibited while their body weight loss was alleviated. We envision that our hydrogelator-assisted assembly strategy could be applied to enhance the therapeutic effects of more drugs, while in the meantime alleviating their adverse effects in the future.

Chemical Communications (Cambridge, United Kingdom) 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

Pryyma, Alla published the artcileRapid, high-yielding solid-phase synthesis of cathepsin-B cleavable linkers for targeted cancer therapeutics, Recommanded Product: 2-Chlorotrityl chloride, the publication is Bioconjugate Chemistry (2020), 31(12), 2685-2690, database is CAplus and MEDLINE.

Antibody-drug conjugates (ADCs) constitute an emerging class of anticancer agents that deliver potent payloads selectively to tumors while avoiding systemic toxicity associated with conventional chemotherapeutics. Critical to ADC development is a serum-stable linker designed to decompose inside targeted cells thereby releasing the toxic payload. A protease-cleavable linker comprising a valine-citrulline (Val-Cit) motif has been successfully incorporated into three FDA-approved ADCs and is found in numerous preclin. candidates. Herein, we present a high-yielding and facile synthetic strategy for a Val-Cit linker that avoids extensive protecting group manipulation and laborious chromatog. associated with previous syntheses and provides yields that are up to 10-fold higher than by standard methods. This method is easily scalable and takes advantage of cost-effective coupling reagents and high loading 2-chlorotrityl chloride (2-CTC) resin. Modularity allows for introduction of various conjugation handles in final stages of the synthesis. Facile access to such analogs serves to expand the repertoire of available enzymically cleavable linkers for ADC generation. This methodol. empowers a robust and facile library generation and future exploration into linker analogs containing unnatural amino acids as a selectivity tuning tool.

Bioconjugate 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

MacSweeney, Aengus published the artcileDiscovery and Structure-Based Optimization of Adenain Inhibitors, Recommanded Product: 2-Chlorotrityl chloride, the publication is ACS Medicinal Chemistry Letters (2014), 5(8), 937-941, database is CAplus and MEDLINE.

The cysteine protease adenain is the essential protease of adenovirus and, as such, represents a promising target for the treatment of ocular and other adenoviral infections. Through a concise two-pronged hit discovery approach we identified tetrapeptide nitrile 1 and pyrimidine nitrile 2 as complementary starting points for adenain inhibition. These hits enabled the first high-resolution X-ray cocrystal structures of adenain with inhibitors bound and revealed the binding mode of 1 and 2. The screening hits were optimized by a structure-guided medicinal chem. strategy into low nanomolar drug-like inhibitors of adenain.

ACS 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 C19H14Cl2, Recommanded Product: 2-Chlorotrityl chloride.

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

Staderini, Matteo published the artcileA tripod anchor offers improved robustness of peptide-based electrochemical biosensors, Product Details of C19H14Cl2, the publication is Sensors and Actuators, B: Chemical (2018), 662-667, database is CAplus.

Peptide-based electrochem. biosensors have proven to be powerful sensing strategies for the detection of proteases and offer a highly versatile system, as simple tuning of the immobilized substrate peptide leads to a new sensing platform. The most common immobilization strategy of peptides onto an electrode surface is via a self-assembled monolayer (SAM) through a thiol group that can be readily chem. incorporated in the target peptide. However, the successful application of these platforms in complex biol. samples can be frustrated by the lack of stability of the peptide-based SAM, that can lead to false positives and limited shelf-life. Herein, we investigated the stability of a peptide-based electrochem. platform endowed with a single or a tribranched thiol group for attaching onto the electrode surface. Side-by-side comparison demonstrated that the tripod anchor generated a highly robust peptide-based electrochem. biosensor that showed improved stability when compared to the monoanchor analog, simplifying data anal. and interpretation, while showing efficient protease detection and similar sensing capabilities.

Sensors and Actuators, B: Chemical 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 C10H10O3, Product Details of C19H14Cl2.

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

Mahindra, Amit published the artcileAntiplasmodial activity of short peptide-based compounds, COA of Formula: C19H14Cl2, the publication is RSC Advances (2015), 5(29), 22674-22684, database is CAplus.

Three series of short peptide-based compounds were synthesized, which upon evaluation against chloroquine-sensitive (D6) and chloroquine-resistant (W2) strains of Plasmodium falciparum in vitro, produced IC₅₀ values ranging between 1.4-4.7 μg mL^-1. Importantly, higher antimalarial activity against the drug-resistant strain of P. falciparum (W2) was observed for the tested peptides, indicating their potential in the treatment of drug-resistant malaria parasites. The lack of cytotoxicity in all tested peptides provides evidence of their safety profile. The selected peptides were evaluated in an enzymic inhibitory assay against plasmepsin II, a potential target for antiplasmodial activity, also indicated from the results of the mol. docking studies.

RSC Advances 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

Rzuczek, Suzanne G. published the artcileFeatures of Modularly Assembled Compounds That Impart Bioactivity Against an RNA Target, Related Products of chlorides-buliding-blocks, the publication is ACS Chemical Biology (2013), 8(10), 2312-2321, database is CAplus and MEDLINE.

Transcriptomes provide a myriad of potential RNAs that could be the targets of therapeutics or chem. genetic probes of function. Cell-permeable small mols., however, generally do not exploit these targets, owing to the difficulty in the design of high affinity, specific small mols. targeting RNA. As part of a general program to study RNA function using small mols., we designed bioactive, modularly assembled small mols. that target the noncoding expanded RNA repeat that causes myotonic dystrophy type 1 (DM1), r-(CUG)^exp. Herein, we present a rigorous study to elucidate features in modularly assembled compounds that afford bioactivity. Different modular assembly scaffolds were investigated, including polyamines, α-peptides, β-peptides, and peptide tertiary amides (PTAs). On the basis of activity as assessed by improvement of DM1-associated defects, stability against proteases, cellular permeability, and toxicity, we discovered that constrained backbones, namely, PTAs, are optimal. Notably, we determined that r-(CUG)^exp is the target of the optimal PTA in cellular models and that the optimal PTA improves DM1-associated defects in a mouse model. Biophys. analyses were employed to investigate potential sources of bioactivity. These investigations show that modularly assembled compounds have increased residence times on their targets and faster on rates than the RNA-binding modules from which they were derived. Moreover, they have faster on rates than the protein that binds r-(CUG)^exp, the inactivation of which gives rise to DM1-associated defects. These studies provide information about features of small mols. that are programmable for targeting RNA, allowing for the facile optimization of therapeutics or chem. probes against other cellular RNA targets.

ACS Chemical Biology 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, Related Products of chlorides-buliding-blocks.

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

Larsson, Malin published the artcileIdentification of potential aryl hydrocarbon receptor ligands by virtual screening of industrial chemicals, Application In Synthesis of 42074-68-0, the publication is Environmental Science and Pollution Research (2018), 25(3), 2436-2449, database is CAplus and MEDLINE.

We have developed a virtual screening procedure to identify potential ligands to the aryl hydrocarbon receptor (AhR) among a set of industrial chems. AhR is a key target for dioxin-like compounds, which is related to these compounds’ potential to induce cancer and a wide range of endocrine and immune system-related effects. The virtual screening procedure included an initial filtration aiming at identifying chems. with structural similarities to 66 known AhR binders, followed by 3 enrichment methods run in parallel. These include two ligand-based methods (structural fingerprints and nearest neighbor anal.) and one structure-based method using an AhR homol. model. A set of 6445 commonly used industrial chems. was processed, and each step identified unique potential ligands. Seven compounds were identified by all three enrichment methods, and these compounds included known activators and suppressors of AhR. Only approx. 0.7% (41 compounds) of the studied industrial compounds was identified as potential AhR ligands and among these, 28 compounds have to our knowledge not been tested for AhR-mediated effects or have been screened with low purity. We suggest assessment of AhR-related activities of these compounds and in particular 2-chlorotrityl chloride, 3-p-hydroxyanilino-carbazole, and 3-(2-chloro-4-nitrophenyl)-5-(1,1-dimethylethyl)-1,3,4-oxadiazol-2(3H)-one.

Environmental Science and Pollution Research 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, Application In Synthesis of 42074-68-0.

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

Kapp, Tobias G. published the artcileModification and functionalization of the guanidine group by tailor-made precursors, Application In Synthesis of 42074-68-0, the publication is Journal of Visualized Experiments (2017), e54873/1-e54873/7, database is CAplus and MEDLINE.

The guanidine group is one of the most important pharmacophoric groups in medicinal chem. The only amino acid carrying a guanidine group is arginine. In this article, an easy method for the modification of the guanidine group in peptidic ligands is provided, with an example of RGD-binding integrin ligands. It was recently demonstrated that the distinct modification of the guanidine group in these ligands allows for the selective modulation of the subtype (e.g., between the subtypes αv and α5). Moreover, a formerly unknown strategy for the functionalization via the guanidine group was demonstrated, and the synthetic approach is reviewed in this document. The modifications described here involve terminally (Nω) alkylated and acetylated guanidine groups. For the synthesis, tailor-made precursor mols. are synthesized, which are then subjected to a reaction with an orthogonally deprotected amine to transfer the pre-modified guanidine group. For the synthesis of alkylated guanidines, precursors based on N,N′-Di-Boc-1H-pyrazole-1-carboxamidine are used to synthesize acylated compounds, the precursor of choice being a correspondingly acylated derivative of N-Boc-S-methylisothiourea, which can be obtained in one- and two-step reactions.

Journal of Visualized Experiments 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, Application In Synthesis of 42074-68-0.

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

Ahlers, Patrick published the artcileDynamic Light Scattering Investigation of the Kinetics and Fidelity of Supramolecular Copolymerizations in Water, Category: chlorides-buliding-blocks, the publication is Macromolecules (Washington, DC, United States) (2017), 50(19), 7712-7720, database is CAplus.

The self-assembly of supramol. copolymers facilitates the preparation of multifunctional materials, with tunable mech., electronic, or bioactive properties. Compared to covalent copolymerization protocols, controlling the mol. weight, stability, and monomer sequence of a multicomponent supramol. copolymer remains limited. Here, we report a light scattering investigation of the charge-regulated supramol. copolymerization in neutral buffer of physiol. ionic strength, supported with electron microscopy and CD spectroscopy experiments Dendritic anionic and cationic peptide comonomers self-assemble into AB-type heterocopolymers with a nanorod-like morphol., a thickness of 11 nm, and a mean length of up to 70 nm. The fidelity in the copolymerization is remarkably high, and excess of either monomer of up to 50 mol % in the feed ratio does not lead to chain stoppering. The narrow length distribution of the copolymers (D < 1.3) and high colloidal stability in physiol. buffer support their applications as biomedical carrier materials.

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, Category: chlorides-buliding-blocks.

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

Spengler, Jan published the artcileUse of an Internal Reference for the Quantitative HPLC-UV Analysis of Solid-Phase Reactions: A Case Study of 2-Chlorotrityl Chloride Resin, HPLC of Formula: 42074-68-0, the publication is ACS Combinatorial Science (2013), 15(5), 229-234, database is CAplus and MEDLINE.

Here we evaluated the use of internal reference compounds for the rapid assessment of reactions performed in solid-phase. An internal reference compound (com. available) was bound to the resin, together with the substrate, and cleaved with the products after completion of the reaction. The peak area of the reference compound in the HPLC-UV chromatograms can be correlated directly with those of other compounds present in the reaction mixture, thereby allowing a quant. interpretation of the chromatograms with respect to conversion and yield. The usefulness of this method was demonstrated by optimization of a protocol for the synthesis of proline-based tripeptides.

ACS Combinatorial Science 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 C14H14, HPLC of Formula: 42074-68-0.

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