Category: 42074-68-0

Gadakh, Bharat published the artcileBase substituted 5′-O-(N-isoleucyl)sulfamoyl nucleoside analogs as potential antibacterial agents, HPLC of Formula: 42074-68-0, the publication is Bioorganic & Medicinal Chemistry (2014), 22(10), 2875-2886, database is CAplus and MEDLINE.

Aminoacyl-sulfamoyl adenosines are well-known nano-molar inhibitors of the corresponding prokaryotic and eukaryotic tRNA synthetases in vitro. Inspired by the aryl-tetrazole containing compounds of Cubist Pharmaceuticals and the modified base as found in the natural antibiotic albomycin, the selectivity issue of the sulfamoylated adenosines prompted us to investigate the pharmacophoric importance of the adenine base. We therefore synthesized and evaluated several isoleucyl-sulfamoyl nucleoside analogs with either uracil, cytosine, hypoxanthine, guanine, 1,3-dideaza-adenine (benzimidazole) or 4-nitro-benzimidazole as the heterocyclic base. Based on the structure and antibacterial activity of microcin C, we also prepared their hexapeptidyl conjugates in an effort to improve their uptake potential. We further compared their antibacterial activity with the parent isoleucyl-sulfamoyl adenosine (Ile-SA), both in in vitro and in cellular assays. Surprisingly, the strongest in vitro inhibition was found for the uracil containing analog. Unfortunately, only very weak growth inhibitory properties were found as of low uptake. The results are discussed in the light of previous literature findings.

Bioorganic & Medicinal 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, HPLC of Formula: 42074-68-0.

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

Xu, Rong published the artcilePeptide-cross-linked protein-imprinted polymers: easy template removal and excellent imprinting effect, Quality Control of 42074-68-0, the publication is CCS Chemistry (2019), 1(5), 544-552, database is CAplus.

Mol. imprinting of proteins remains a huge challenge because of two major obstacles: difficulty in template removal and low imprinting efficiency. Herein, we propose a new strategy to simultaneously overcome these two challenges by creating molecularly imprinted polymers (MIPs) with nanoscale shape-memorable imprint cavities. These novel MIPs were developed by simply crosslinking the polymers with a peptide cross-linker instead of commonly used cross-linkers. Due to the unique pH-induced helix- coil transition of the peptide cross-linker, adjusting the pH from 5.5 to 7.4 leads to an expansion of the imprint cavities, thus facilitating template removal. Returning the pH back to 5.5 restores the original size and shape of the imprint cavities due to the precise refolding of peptide. A template protein can therefore be readily removed under mild conditions, while simultaneously achieving a significantly improved imprinting effect.

CCS 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 C7H3IN2O2, Quality Control of 42074-68-0.

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

Corpas-Lopez, Victoriano published the artcileO-Alkyl Hydroxamates Display Potent and Selective Antileishmanial Activity, Related Products of chlorides-buliding-blocks, the publication is Journal of Medicinal Chemistry (2020), 63(11), 5734-5751, database is CAplus and MEDLINE.

Leishmania (L.) infantum causes visceral, cutaneous, and mucosal leishmaniasis in humans and canine leishmaniasis in dogs. Herein, we describe that O-alkyl hydroxamate derivatives displayed potent and selective in vitro activity against the amastigote stage of L. infantum while no activity was observed against promastigotes. Compound PhNHCO(CH₂)₆CONHOCPh₃ (I)showed potent in vivo activity against L. infantum. Moreover, the combination of compound 5 supported on gold nanoparticles and meglumine antimoniate was also effective in vivo and improved the activity of these compounds compared to that of the individual treatment. Docking studies showed that compound 5 did not reach highly conserved pocket C and established interactions with the semiconserved residues V44, A45, R242, and E243 in pocket A of LiSIR2rp1. The surface space determined by these four amino acids is not conserved in human sirtuins. Compound I represents a new class of selective ligands with antileishmanial activity.

Journal of Medicinal 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, Related Products of chlorides-buliding-blocks.

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

Koronkiewicz, Brian published the artcileShallow distance dependence for proton-coupled tyrosine oxidation in oligoproline peptides, Application In Synthesis of 42074-68-0, the publication is Journal of the American Chemical Society (2020), 142(28), 12106-12118, database is CAplus and MEDLINE.

We have explored the kinetic effect of increasing electron transfer (ET) distance in a biomimetic, proton-coupled electron-transfer (PCET) system. Biol. ET often occurs simultaneously with proton transfer (PT) in order to avoid the high-energy, charged intermediates resulting from the stepwise transfer of protons and electrons. These concerted proton-electron-transfer (CPET) reactions are implicated in numerous biol. ET pathways. In many cases, PT is coupled to long-range ET. While many studies have shown that the rate of ET is sensitive to the distance between the electron donor and acceptor, extensions to biol. CPET reactions are sparse. The possibility of a unique ET distance dependence for CPET reactions deserves further exploration, as this could have implications for how we understand biol. ET. We therefore explored the ET distance dependence for the CPET oxidation of tyrosine in a model system. We prepared a series of metallopeptides with a tyrosine separated from a Ru(bpy)₃²⁺ complex by an oligoproline bridge of increasing length. Rate constants for intramol. tyrosine oxidation were measured using the flash-quench transient absorption technique in aqueous solutions The rate constants for tyrosine oxidation decreased by 125-fold with three added proline residues between tyrosine and the oxidant. By comparison, related intramol. ET rate constants in very similar constructs were reported to decrease by 4-5 orders of magnitude over the same number of prolines. The observed shallow distance dependence for tyrosine oxidation is proposed to originate in part from the requirement for stronger oxidants, leading to a smaller hole-transfer effective tunneling barrier height. The shallow distance dependence observed here and extensions to distance-dependent CPET reactions have potential implications for long-range charge transfers.

Journal of the American Chemical Society 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

Al Musaimi, Othman published the artcileCombining solid phase synthesis and chromatographic purification for efficient peptide manufacture, Application In Synthesis of 42074-68-0, the publication is Chimica Oggi (2020), 38(2), 18-21, database is CAplus.

In recent years, peptides have gained an important position in the drug arena for a variety of treatments. Solid-phase peptide synthesis (SPPS) continues to have a significant impact in both R&D as well as in production of com. peptides. The combination of SPPS with reverse-phase (RP) chromatog. separations allowed for the peptides to be purified to levels suitable for drug usage. Thanks to their chem. and phys. stability to high pressure, chems., temperature and oxidising reagents, polystyrene / divinyl benzene (PS/DVB) resins are the main solid support for peptide synthesis as well as being suitable for the chromatog. purification of the peptides by RP and ion exchange (IEX). Depending on the application, the optimal crosslinking changes, as do the optimal particle size, the uniformity in particle size distribution and the porosity of the resin. The characteristics and applications of the PS/DVB resins are explored in this paper for the synthesis and purification of peptides of com. interest.

Chimica Oggi 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

Kuang, Jing published the artcileiRGD Modified Chemo-immunotherapeutic Nanoparticles for Enhanced Immunotherapy against Glioblastoma, Application of 2-Chlorotrityl chloride, the publication is Advanced Functional Materials (2018), 28(17), n/a, database is CAplus.

Glioblastoma is the most common primary brain tumor in adults and still remains incurable, due to the limited accumulation of drugs in the tumor area. Herein, iRGD-modified nanoparticles, DOX@MSN-SS-iRGD&1MT, are developed for simultaneous delivery of chemotherapeutic agents (doxorubicin, DOX) and immune checkpoint inhibitor (1-methyltryptophan, 1MT) into orthotopic glioma. The nanoparticles are comprised of mesoporous silica nanoparticles loaded with DOX, combined with Asp-Glu-Val-Asp (DEVD) connected 1MT, and finally modified by iRGD. These nanoparticles show the capability of penetrating through blood brain barrier into the tumor area, and significantly improve accumulation of drugs in orthotopic brain tumors with minimal side effects. The nanoparticles also activate cytotoxic CD8⁺ T lymphocytes and inhibit CD4⁺ T cells in both GL261 cells cocultured with splenocytes in vitro and GL261-luc orthotopic tumors in vivo. Moreover, the expression of antitumor cytokines IFNα/β, IFN-γ, TNF, IL-17, STING, and GrzB is upregulated while protumor proteins p-STAT3 and IL-10 are downregulated in the brain tumor area. This study demonstrates the advantages of chemo-immunotherapeutic nanoparticles accumulated in the brain tumor area and their effectively inhibiting tumor proliferation, which establishes a delivery platform to promote antitumor immunity against glioblastoma.

Advanced Functional Materials 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 of 2-Chlorotrityl chloride.

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

Lunagariya, Jignesh published the artcileDesign and synthesis of analogues of marine natural product galaxamide, an N-methylated cyclic pentapeptide, as potential anti-tumor agent in vitro, HPLC of Formula: 42074-68-0, the publication is Marine Drugs (2016), 14(9), 161/1-161/22, database is CAplus and MEDLINE.

Herein, we report design and synthesis of novel 26 galaxamide analogs with N-methylated cyclo-pentapeptide, and their in vitro anti-tumor activity towards the panel of human tumor cell line, such as, A549, A549/DPP, HepG2 and SMMC-7721 using MTT assay. We have also investigated the effect of galaxamide and its representative analogs on growth, cell-cycle phases, and induction of apoptosis in SMMC-7721 cells in vitro. Reckon with the significance of conformational space and N-Me aminoacid (aa) comprising this compound template, we designed the analogs with modification in N-Me-aa position, change in aa configuration from l to d aa and substitute one Leu-aa to d/l Phe-aa residue with resp. to the parent structure. The efficient solid phase parallel synthesis approach is employed for the linear pentapeptide residue containing N-Me aa, followed by solution phase macrocyclisation to afford target cyclo pentapeptide compounds In the present study, all galaxamide analogs exhibited growth inhibition in A549, A549/DPP, SMMC-7721 and HepG2 cell lines. Compounds 6, 18, and 22 exhibited interesting activities towards all cell line tested, while Compounds 1, 4, 15, and 22 showed strong activity towards SMMC-7221 cell line in the range of 1-2 μg/mL IC50. Flow cytometry experiment revealed that galaxamide analogs namely Compounds 6, 18, and 22 induced concentration dependent SMMC-7721 cell apoptosis after 48 h. These compounds induced G0/G1 phase cell-cycle arrest and morphol. changes indicating induction of apoptosis. Thus, findings of our study suggest that the galaxamide and its analogs 6, 18 and 22 exerted growth inhibitory effect on SMMC-7721 cells by arresting the cell cycle in the G0/G1 phase and inducing apoptosis. Compound 1 showed promising anti-tumor activity towards SMMC-7721 cancer cell line, which is 9 and 10 fold higher than galaxamide and reference DPP (cisplatin), resp.

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, HPLC of Formula: 42074-68-0.

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

Kumeria, Tushar published the artcilePhotoswitchable Membranes Based on Peptide-Modified Nanoporous Anodic Alumina: Toward Smart Membranes for On-Demand Molecular Transport, Computed Properties of 42074-68-0, the publication is Advanced Materials (Weinheim, Germany) (2015), 27(19), 3019-3024, database is CAplus and MEDLINE.

This study presents for the first time, a photo stimuli responsive membrane system based on NAAMs functionalized with an azobenzene-containing photoswitchable peptide (PSP). PSP mols. were selectively immobilized along the internal surface of the nanoporous anodic alumina membranes (NAAM) pores, in order to manipulate the effective pore diameter of the NAAMs, depending on their isomeric form. This pore diameter modulation then regulates the transport of model dye mol. (Rose Bengal (RosB)) across the PSP modified NAA membranes. Exposure to specific wavelengths of light (364 nm in this case) switches the azobenzene component of PSP from a trims to a cis isomer, such that the associated, change in PSP geometry controls the pore diameter of NAAMs and hence the selective transport of RosB.

Advanced Materials (Weinheim, Germany) 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, Computed Properties of 42074-68-0.

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

Jeong, Hyeri published the artcileEfficient Synthesis and Characterization of Monoprotected Symmetrical Poly(Ethylene Glycol) Diamine, HPLC of Formula: 42074-68-0, the publication is Bulletin of the Korean Chemical Society (2018), 39(1), 29-32, database is CAplus.

Solid-phase synthesis of monoprotected poly(ethylene glycol) (PEG) diamine is demonstrated. 2-Chlorotrityl chloride (2-CTC) resin was used as a solid support for inducing monofunctionalization using excess PEG diamine. Fmoc-monoprotected PEG was prepared from 2-CTC resin and fully characterized by high-performance liquid chromatog. and electrospray ionization mass spectrometry. We envision that this strategy will provide an efficient method of preparing various kinds of heterobifunctional PEG mols. without a need for further purification steps.

Bulletin of the Korean Chemical Society 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, HPLC of Formula: 42074-68-0.

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

Miao, Qingqing published the artcileNear-Infrared Fluorescent Molecular Probe for Sensitive Imaging of Keloid, Safety of 2-Chlorotrityl chloride, the publication is Angewandte Chemie, International Edition (2018), 57(5), 1256-1260, database is CAplus and MEDLINE.

Early detection of skin diseases is imperative for their effective treatment. However, fluorescence mol. probes that allow this are rare. The first activatable near-IR (NIR) fluorescent mol. probe is reported for sensitive imaging of keloid cells, skin cells from abnormal scar fibrous lesions. As keloid cells have high expression levels of fibroblast activation protein-alpha (FAPα), the probe (FNP1) is designed to have a caged NIR dye and a FAPα-cleavable peptide substrate linked by a self-immolative segment. FNP1 can quickly and specifically turn on its fluorescence at 710 nm by 45-fold in the presence of FAPα, allowing it to effectively recognize keloid cells from normal skin cells. Integration of FNP1 with a simple microneedle-assisted topical application enables sensitive detection of keloid cells in metabolically-active human skin tissue with a theor. limit of detection down to 20 000 cells.

Angewandte Chemie, International Edition 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, Safety of 2-Chlorotrityl chloride.

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