74489-49-9

Upstream product

• 31499-54-4 4-azidobenzyl alcohol 
• 623-04-1 4-aminobenzenemethanol 
• 2101-86-2 p-methylazidobenzene 
• 589-15-1 1-bromomethyl-4-bromobenzene 
• 619-73-8 4-nitrobenzyl chloride 
• 106-49-0 p-toluidine 
• 1067169-70-3 4-azidobenzyl mesylate 

Downstream Products

• 136057-08-4 C₁₇H₁₉N₃O₃ 
• 136057-07-3 1-Azido-4-(2-benzyloxy-ethoxymethyl)-benzene 
• 92001-72-4 1-(4-azidobenzyl)adenine 
• 85107-83-1 N⁶-(p-azidobenzyl)adenosine 
• 62133-08-8 C₁₅H₁₀N₄O₂ 
• 1162643-37-9 N-(4-azidobenzyl)-N-(2-[3,4-bis(tert-butyldimethylsilyloxy)phenyl]ethyl)amine 
• 1219081-19-2 1-(4-azidophenylmethyl)-1H-benzotriazole 
• 1219081-29-4 2-(4-azidophenylmethyl)-2H-benzotriazole 
• 1215305-61-5 C₂₆H₃₄N₄O₅Si 
• 1227005-52-8 (5RS)-5-(4-azidobenzyloxy)-N-(2-trimethylsilyl)ethoxycarbonyl-1,2,5,6-tetrahydropyridine 
• 1352807-09-0 1-azido-4-(azidomethyl)benzene 
• 1352807-22-7 1-[4-(azidomethyl)phenyl]-4,5,6,7-tetrahydro-1H-benzo[d][1,2,3]triazole 
• 1449329-04-7 1-azido-4-((pent-4-yn-1-yloxy)methyl)benzene 

Relevant academic research and scientific papers

BIOPROBES FOR LYSYL OXIDASES AND USES THEREOF

The present invention relates to novel bioprobes which are capable of binding to certain amine oxidase enzymes. These bioprobes are useful in methods of detecting and determining the concentration of certain amine oxidase enzymes in a sample as well as in methods for the quantitative assessment of inhibition of certain amine oxidases.

SELECTIVE DRUG RELEASE FROM INTERNALIZED CONJUGATES OF BIOLOGICALLY ACTIVE COMPOUNDS

The invention relates to conjugates of biologically active compounds, wherein such a conjugate is comprised of a sequence of amino acids containing a tripeptide that confers selective cleavage by tumor tissue homogenate for release of free drug and/or imp

Highly efficient synthesis of silica-coated magnetic nanoparticles modified with iminodiacetic acid applied to synthesis of 1,2,3-triazoles

Great efforts have been made to discover new catalysts to facilitate synthesis of organic fine chemicals. In this research, a new silica-coated magnetic nanoparticles functionalized by iminodiacetic acid (Fe3O4@SiO2@IDA) w

Triazolidinyl-containing hydrophobic adamantane type selective androgen receptor depressant and preparation method thereof

The invention discloses triazolidinyl-containing adamantane type chimeric molecules as well as a preparation method and application thereof as selective androgen receptor (AR) depressants in the fieldof preventing cancer related to high expression of androgen receptors, and belongs to the field of medicine chemistry. The molecules have structural formulae (I, II) shown in the description. According to the molecules, an AR protein micromolecule antagonist and a hydrophobic label ligand adamantly are connected through connecting arms to obtain bifunctional small molecules, and the molecules areselective androgen receptor depressants which are capable of selectively inducing AR protein degradation. The bifunctional small molecules provided by the invention, and medicine combinations of thebifunctional small molecules, have wide application in treating prostate cancer, advanced prostate cancer, castrated refractory prostate cancer or stomach cancer, breast cancer, other high androgenicskin diseases, Kennedy's disease and amyotrophic lateral sclerosis (ALS).

Phthalimide selective androgen receptor degradation agent as well as preparation method and application thereof

The invention discloses phthalimide chimeric molecules containing 1, 2, 3-triazolyl, a preparation method of the phthalimide chimeric molecules and application of the phthalimide chimeric molecules serving as selective androgen receptor (AR) inhibitors in the field of AR high-expression cancer resistance, and belongs to the field of medicinal chemistry. The compounds have a structural general formula disclosed in the invention; the compounds have a good binding effect on AR, have AR degradation activity, and can be used as candidates for further development or lead compounds for preparing anti-AR-high-expression cancer drugs.

A2B Adenosine Receptor Antagonists with Picomolar Potency

The A2B adenosine receptor (A2BAR) was proposed as a novel target for the (immuno)therapy of cancer since A2BAR blockade results in antiproliferative, antiangiogenic, antimetastatic, and immunostimulatory effects. In this study, we explored the structure-activity relationships of xanthin-8-yl-benzenesulfonamides mainly by introducing a variety of linkers and substituents attached to the sulfonamide residue. A new, convergent strategy was established, which facilitated the synthesis of the target compounds. Many of the new compounds exhibited subnanomolar affinity for the A2BAR combined with high selectivity. Functional groups were introduced, which will allow the attachment of dyes and other reporter groups. 8-(4-((4-(4-Bromophenyl)piperazin-1-yl)sulfonyl)phenyl)-1-propylxanthine (34, PSB-1901) was the most potent A2B-antagonist (Ki 0.0835 nM, KB 0.0598 nM, human A2BAR) with >10 000-fold selectivity versus all other AR subtypes. It was similarly potent and selective at the mouse A2BAR, making it a promising tool for preclinical studies. Computational studies predicted halogen bonding to contribute to the outstanding potency of 34.

A Dual-Response Fluorescent Probe for the Detection of Viscosity and H2S and Its Application in Studying Their Cross-Talk Influence in Mitochondria

Intracellular viscosity is an essential microenvironmental parameter and H2S is a critical gaseous signaling molecule, which are both related to various physiological processes. It is reported that the change of viscosity and an imbalance of H2S production in the mitochondria are both associated with overexpression of amyloid betapeptide (Aβ), which is thought to play a central role in the pathogenesis of Alzheimer's disease (AD). However, to our best knowledge, no fluorescent probe is found for dual detection of mitochondrial viscosity and H2S. Herein, a dual-response fluorescent probe (Mito-VS) is designed and synthesized to monitor the level of viscosity and H2S, respectively. Mito-VS itself is nonfluorescent due to a free intramolecular rotation between dimethylaniline and pyridine. After the increase of viscosity, the rotation is prohibited and an intense red fluorescence is released. Upon the addition of H2S, the probe can react with H2S to form compound 3 and a strong green fluorescence can be observed. Moreover, the probe possesses a good mitochondrion-targeting ability and is applied for imaging the change of viscosity on the red channel and visualizing the variation of exogenous and endogenous H2S concentration on the green channel in mitochondria. Most importantly, the probe is capable of studying the cross-talk influence of viscosity and H2S in mitochondria, which is very beneficial for knowing the pathogenesis of AD.

Fluorescent probe for specifically identifying hydrogen sulfide

The invention discloses a fluorescent probe for specifically identifying hydrogen sulfide. The molecular structural formula of the fluorescent probe is expressed as a formula which is as shown in thedescription. When the fluorescent probe acts with hydrog

Synthesis of photophore and fluorophore modified o-benzylserine derivatives

O-Benzylation of serine is one of the important protection methods for solid phase peptide synthesis. The utilities of the protection group may be indicated that chemical modifications for O-benzylserine will be utilized to make functional peptides on sol

A General Strategy Toward Highly Fluorogenic Bioprobes Emitting across the Visible Spectrum

A general approach toward highly fluorogenic probes across the visible spectrum for various analytes offers significant potential for engineering a wide range of bioprobes with diverse sensing and imaging functions. Here we show a facile and general strategy that involves introducing a new fluorogenic mechanism in boron dipyrromethene (BODIPY) dyes, based on the principle of stimuli-triggered dramatic reduction in the electron-withdrawing capabilities of the meso-substituents of BODIPYs. The fluorogenic mechanism has been demonstrated to be applicable in various BODIPYs with emission maxima ranging from green to far red (509, 585, and 660 nm), and the synthetic strategy allows access to a panel of highly fluorogenic bioprobes for various biomolecules and enzymes (H2O2, H2S, and protease) via introducing specific triggering motifs. The potency of the general design strategy is exemplified by its application to develop a mitochondria-targeting far-red probe capable of imaging of endogenous H2O2 in living cells.