Tag: M.W=300-350

Areephong, Jetsuda published the artcileThree-state photochromic switching in a silyl bridged diarylethene dimer, COA of Formula: C15H14Cl2S2, the publication is Organic & Biomolecular Chemistry (2007), 5(8), 1170-1174, database is CAplus and MEDLINE.

The synthesis and photochem. characterization of bicomponent mol. switches based on covalently tethered dithienylethene photochromes is described. Both photochromic units undergo complete switching between the fully cyclized and fully non-cyclized states despite a significant level of electronic communication between the individual units and their proximity.

Organic & Biomolecular Chemistry published new progress about 219537-97-0. 219537-97-0 belongs to chlorides-buliding-blocks, auxiliary class Fused/Partially Saturated Cycles,Cyclopentenes, name is 5-Chloro-3-[2-(5-chloro-2-methylthien-3-yl)cyclopent-1-en-1-yl]-2-methylthiophene, and the molecular formula is C15H14Cl2S2, COA of Formula: C15H14Cl2S2.

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

Huo, Yuantao published the artcileDelivering bioactive cyclic peptides that target Hsp90 as prodrugs, SDS of cas: 42074-68-0, the publication is Journal of Enzyme Inhibition and Medicinal Chemistry (2019), 34(1), 728-739, database is CAplus and MEDLINE.

The most challenging issue facing peptide drug development is producing a mol. with optimal phys. properties while maintaining target binding affinity. Masking peptides with protecting groups that can be removed inside the cell, produces a cell-permeable peptide, which theor. can maintain its biol. activity. Described are series of prodrugs masked using: (a) O-alkyl, (b) N-alkyl, and (c) acetyl groups, and their binding affinity for Hsp90. Alkyl moieties increased compound permeability, P_app, from 3.3 to 5.6, however alkyls could not be removed by liver microsomes or in-vivo and their presence decreased target binding affinity (IC₅₀ of ≥10μM). Thus, unlike small mols., peptide masking groups cannot be predictably removed; their removal is related to the 3-D conformation. O-acetyl groups were cleaved but are labile, increasing challenges during synthesis. Utilizing acetyl groups coupled with mono-methylated amines may decrease the polarity of a peptide, while maintaining binding affinity.

Journal of Enzyme Inhibition and 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, SDS of cas: 42074-68-0.

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

Kubyshkin, Vladimir published the artcileExploring hydrophobicity limits of polyproline helix with oligomeric octahydroindole-2-carboxylic acid, Synthetic Route of 42074-68-0, the publication is Journal of Peptide Science (2018), 24(4-5), n/a, database is CAplus and MEDLINE.

The polyproline-II helix is the most extended naturally occurring helical structure and is widely present in polar, exposed stretches and “unstructured” denatured regions of polypeptides. Can it be hydrophobic. In this study, we address this question using oligomeric peptides formed by a hydrophobic proline analog, (2S,3aS,7aS)-octahydroindole-2-carboxylic acid (Oic). Previously, we found the mol. principles underlying the structural stability of the polyproline-II conformation in these oligomers, whereas the hydrophobicity of the peptide constructs remains to be examined Therefore, we investigated the octan-1-ol/water partitioning and inclusion in detergent micelles of the oligo-Oic peptides. The results showed that the hydrophobicity is remarkably enhanced in longer oligomeric sequences, and the oligo-Oic peptides with 3 to 4 residues and higher are specific towards hydrophobic environments. This contrasts significantly to the parent oligoproline peptides, which were moderately hydrophilic. With these findings, we have demonstrated that the polyproline-II structure is compatible with nonpolar media, whereas addnl. manipulations of the terminal functionalities feature solubility in extremely nonpolar solvents such as hexane.

Journal of Peptide 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 C19H14Cl2, Synthetic Route of 42074-68-0.

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

Wilson, Danielle published the artcileTurning “On” and “Off” a Pyridoxal 5′-Phosphate Mimic Using Light, Product Details of C15H14Cl2S2, the publication is Angewandte Chemie, International Edition (2012), 51(22), 5431-5434, S5431/1-S5431/13, database is CAplus and MEDLINE.

The use of light to reversibly change the structure of biol. relevant mols., thereby turning important biochem. functions “on” and “off” on command, offers a non-invasive, rapid, spatial and temporal tool for research and therapy. The biol. active form of vitamin B₆ is pyridoxal 5′-phosphate (PLP), a versatile enzyme cofactor responsible for amino acid metabolism in all organisms from bacteria to humans. The present work describes the development of a photoresponsive PLP mimic whose catalytic activity can be reversibly switched “on” and “off” by irradiating it with UV and visible light, resp. This was accomplished by taking advantage of the photoswitchable dithienylethene (DTE) architecture, which undergoes UV light-dependent ring-closing and visible light-dependent ring-opening reactions. The ability of this photoresponsive PLP mimic to serve as a controllable catalyst was demonstrated using hydrogen-deuterium exchange experiments and ¹H NMR spectroscopy of solutions of optically pure L-alanine. The relative rates of deuterium exchange reflect the difference in electronic properties of the “ring-open” and “ring-closed” forms of the PLP mimic.

Angewandte Chemie, International Edition published new progress about 219537-97-0. 219537-97-0 belongs to chlorides-buliding-blocks, auxiliary class Fused/Partially Saturated Cycles,Cyclopentenes, name is 5-Chloro-3-[2-(5-chloro-2-methylthien-3-yl)cyclopent-1-en-1-yl]-2-methylthiophene, and the molecular formula is C15H12O8, Product Details of C15H14Cl2S2.

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

Nguyen, Anh Minh Thao published the artcileInfluence of N-methylation and conformation on almiramide anti-leishmanial activity, SDS of cas: 42074-68-0, the publication is Molecules (2021), 26(12), 3606, database is CAplus and MEDLINE.

The almiramide N-methylated lipopeptides exhibit promising activity against trypanosomatid parasites. A structure-activity relationship study has been performed to examine the influences of N-methylation and conformation on activity against various strains of leishmaniasis protozoan and on cytotoxicity. The synthesis and biol. anal. of twenty-five analogs demonstrated that derivatives with a single Me group on either the first or fifth residue amide nitrogen exhibited greater activity than the permethylated peptides and relatively high potency against resistant strains. Replacement of amino amide residues in the peptide, by turn inducing α amino γ lactam (Agl) and N-aminoimidazalone (Nai) counterparts, reduced typically anti-parasitic activity; however, peptide amides possessing Agl residues at the second residue retained significant potency in the unmethylated and permethylated series. Systematic study of the effects of methylation and turn geometry on anti-parasitic activity indicated the relevance of an extended conformer about the central residues, and conformational mobility by tertiary amide isomerization and turn geometry at the extremities of the active peptides.

Molecules 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, SDS of cas: 42074-68-0.

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

Presa, Andreu published the artcilePhotoswitching the Cytotoxic Properties of Platinum(II) Compounds, Formula: C15H14Cl2S2, the publication is Angewandte Chemie, International Edition (2015), 54(15), 4561-4565, database is CAplus and MEDLINE.

The photoactivation of potential anticancer metal complexes is a hot topic of current research as it may lead to the development of more selective drugs. Photoactivated chemotherapy (PACT) with coordination compounds is usually based on a (photo)chem. reaction taking place at the metal center. Herein, a new strategy is exploited that consists of “photomodifying” a ligand coordinated to metal ions. Platinum(II) complexes from photoswitchable 1,2-dithienylethene-containing ligands have been prepared, which exhibit two interconvertible photoisomeric forms that present distinct DNA-interacting properties and cytotoxic behaviors.

Angewandte Chemie, International Edition published new progress about 219537-97-0. 219537-97-0 belongs to chlorides-buliding-blocks, auxiliary class Fused/Partially Saturated Cycles,Cyclopentenes, name is 5-Chloro-3-[2-(5-chloro-2-methylthien-3-yl)cyclopent-1-en-1-yl]-2-methylthiophene, and the molecular formula is C15H14Cl2S2, Formula: C15H14Cl2S2.

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

Wendt, Mathias published the artcileBicyclic β-Sheet Mimetics that Target the Transcriptional Coactivator β-Catenin and Inhibit Wnt Signaling, Safety of 2-Chlorotrityl chloride, the publication is Angewandte Chemie, International Edition (2021), 60(25), 13937-13944, database is CAplus and MEDLINE.

Protein complexes are defined by the three-dimensional structure of participating binding partners. Knowledge about these structures can facilitate the design of peptidomimetics which have been applied for example, as inhibitors of protein-protein interactions (PPIs). Even though β-sheets participate widely in PPIs, they have only rarely served as the basis for peptidomimetic PPI inhibitors, in particular when addressing intracellular targets. Here, we present the structure-based design of β-sheet mimetics targeting the intracellular protein β-catenin, a central component of the Wnt signaling pathway. Based on a protein binding partner of β-catenin, a macrocyclic peptide was designed and its crystal structure in complex with β-catenin obtained. Using this structure, we designed a library of bicyclic β-sheet mimetics employing a late-stage diversification strategy. Several mimetics were identified that compete with transcription factor binding to β-catenin and inhibit Wnt signaling in cells. The presented design strategy can support the development of inhibitors for other β-sheet-mediated PPIs.

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 C8H8O3, Safety of 2-Chlorotrityl chloride.

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

Zhang, Qinghua published the artcileGreen and inexpensive choline-derived solvents for cellulose decrystallization, SDS of cas: 23616-79-7, the publication is Chemistry – A European Journal (2012), 18(4), 1043-1046, S1043/1-S1043/4, database is CAplus and MEDLINE.

Choline acetate was used as a solvent for rapid decrystn. of microcrystalline cellulose (Avicel PH 105). The effect of additives, such as tributylmethylammonium chloride, tributylbenzylammonium chloride and triethylmethylammonium chloride, on solubility and decrystn. degree was assessed. Compared to choline chloride, the use of choline acetate substantially improved the decrystn. rate and could be easily recycled.

Chemistry – A European Journal published new progress about 23616-79-7. 23616-79-7 belongs to chlorides-buliding-blocks, auxiliary class Phase Transfer Catalyst, name is N-Benzyl-N,N-dibutylbutan-1-aminium chloride, and the molecular formula is C14H10O4S2, SDS of cas: 23616-79-7.

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