74489-49-9

Upstream product

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

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 
• 1235579-94-8 phenyl 2-O-(4-azidobenzyl)-3-O-benzyl-4,6-O-benzylidene-1-thio-β-D-glucopyranoside 
• 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 

Relevant academic research and scientific papers

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

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

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.

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.

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

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.

BODIPY-based high-sensitivity fluorescent probe and synthesis method and application thereof

The invention relates to a BODIPY-based high-sensitivity fluorescent probe and a synthesis method and application thereof. A structural general formula of the probe is shown as (I), wherein Trigger is stimulant triggering groups, R1 and R2 are groups for regulating and controlling fluorescent transmission wavelength of the probe and introducing organelle targeting, and R1 and R2 are defined in the description. By the probe, detection of different substrates can be realized without changing mother nucleus structure of the probe by only changing different Trigger groups. In addition, according to different needs on wavelength and targeting, the mother nucleus structure of the probe can be quickly modified. By changing R1 and R2, maximum fluorescent emission wavelength of the probe can be changed, and the probe can target mitochondrion to realize detection of active substances in the mitochondrion. The probe has good biocompatibility, thereby being applicable to detecting biological systems. Application value of the fluorescent probe in the aspect of detecting bioactive molecules and protease over-expressed in inflammatory or tumor tissue has potential social benefit and economic benefit.

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