19717-14-7

Upstream product

• 6917-08-4 N-(4-methylphenyl)-4-nitrobenzamide 
• 18144-47-3 tert-butyl 4-aminobenzoate 
• 1255217-85-6 tert-butyl 4-(4-nitro-benzoylamino)benzoate 
• 62-23-7 4-nitro-benzoic acid 
• 619-45-4 4-methoxycarbonyl aniline 
• 122-04-3 4-nitro-benzoyl chloride 
• 540-23-8 p-toluidine hydrochloride 
• 150-13-0 4-amino-benzoic acid 
• 27126-29-0 N-(4-methoxybenzyl)-4-aminobenzoic acid 
• 4380-38-5 4-(4-methoxy-benzylidenamino)-benzoic acid 
• 887751-39-5 N,N-9-fluorenylmethyloxycarbonyl-(4-methoxybenzyl)-4-aminobenzoic acid 
• 925676-13-7 (4-chlorocarbonyl-phenyl)-(4-methoxy-benzyl)-carbamic acid 9H-fluoren-9-ylmethyl ester 
• 39799-74-1 methyl 4-<(4'-nitrobenzoyl)amino>benzoate 
• 887751-38-4 N-(4-methoxybenzyl)-4-(4-nitrobenzamido)benzoic acid 

Relevant academic research and scientific papers

Scalable Syntheses of Methoxyaspartate and Preparation of the Antibiotic Cystobactamid 861-2 and Highly Potent Derivatives

An improved scalable synthesis of orthogonally functionalized methoxyaspartate, the chiral hinge region element in cystobactamids, is reported. This improvement sets the stage for the total synthesis of four new cystobactamids along with cystobactamid 861

Cystobactamids 920-1 and 920-2: Assignment of the Constitution and Relative Configuration by Total Synthesis

Total synthesis of cystobactamid 920-1 and its epimer has allowed an unambiguous assignment of the relative and absolute configuration of the natural product. A careful structural analysis of each isomer using both NMR and computational techniques also pr

NOVEL CYSTOBACTAMIDE DERIVATIVES

The present invention relates to novel derivatives of cystobactamides of formula (lb) and the use thereof for the treatment or prophylaxis of bacterial infections.

The invention relates to a tree-like molecule for nucleus of molecular imaging probe and its application

The invention relates to a molecular imaging probe taking dendrimer as a core and an application of the molecular imaging probe. A multi-mode and multi-target-point molecular imaging probe with a low steric hindrance is obtained by connecting four rigid a

Total Synthesis and Biological Assessment of Novel Albicidins Discovered by Mass Spectrometric Networking

Natural products represent an important source of potential novel antimicrobial drug leads. Low production by microorganisms in cell culture often delays the structural elucidation or even prevents a timely discovery. Starting from the anti-Gram-negative antibacterial compound albicidin produced by Xanthomonas albilineans, we describe a bioactivity-guided approach combined with non-targeted tandem mass spectrometry and spectral (molecular) networking for the discovery of novel antimicrobial compounds. We report eight new natural albicidin derivatives, four of which bear a β-methoxy cyanoalanine or β-methoxy asparagine as the central α-amino acid. We present the total synthesis of these albicidins, which facilitated the unambiguous determination of the (2 S,3 R)-stereoconfiguration which is complemented by the assessment of the stereochemistry on antibacterial activity.

CYSTOBACTAMIDES

The present invention provides cystobactamides of formula (I) and the use thereof for the treatment or prophylaxis of bacterial infections:

Perturbation of the c-Myc-Max Protein-Protein Interaction via Synthetic α-Helix Mimetics

The rational design of inhibitors of the bHLH-ZIP oncoprotein c-Myc is hampered by a lack of structure in its monomeric state. We describe herein the design of novel, low-molecular-weight, synthetic α-helix mimetics that recognize helical c-Myc in its transcriptionally active coiled-coil structure in association with its obligate bHLH-ZIP partner Max. These compounds perturb the heterodimer's binding to its canonical E-box DNA sequence without causing protein-protein dissociation, heralding a new mechanistic class of "direct" c-Myc inhibitors. In addition to electrophoretic mobility shift assays, this model was corroborated by further biophysical methods, including NMR spectroscopy and surface plasmon resonance. Several compounds demonstrated a 2-fold or greater selectivity for c-Myc-Max heterodimers over Max-Max homodimers with IC50 values as low as 5.6 μM. Finally, these compounds inhibited the proliferation of c-Myc-expressing cell lines in a concentration-dependent manner that correlated with the loss of expression of a c-Myc-dependent reporter plasmid despite the fact that c-Myc-Max heterodimers remained intact. (Chemical Equation Presented).

Design, synthesis and biological evaluation of novel non-peptide boronic acid derivatives as proteasome inhibitors

A series of novel non-peptide boronic acid derivatives were designed and synthesized via rational drug design principles. All target compounds were screened for the proteasome inhibitory activities in vitro. Selected compounds (6a and 7j) were evaluated f

Substituent effects on energetics of peptide-carboxylate hydrogen bonds as studied by 1H NMR spectroscopy: Implications for enzyme catalysis

Substituent effects in N-H···O hydrogen bonds were estimated by comparing the acidities of two series of model compounds: N-benzoylanthranilic acids (A) and 4-benzoylamidobenzoic acids (B). Intramolecular N-H···O hydrogen bonds were found to be present in the A series of compounds, while B acids were used as control models. The respective pKa values for A and B acids were determined experimentally in DMSO solution using proton NMR spectroscopy. With X = H, the pKa for A and B acids were observed to be 7.6 and 11.6, respectively, a difference of 4.0 units (ΔpKa). However, with X = p-NO 2, the ΔpKa value between A and B acids increased to 4.7 units: the pKa values for A and B acids were determined as 6.7 and 11.4, respectively. The ΔpKa values between A and B acids as a function of the X substituents were studied in 10 other examples. The effects of X substituents in A acids could be predicted on the basis of the observed linear Hammett correlations, and the sensitivity of each substituent effect was found to be comparable to those observed for the ionization of substituted benzoic acids (ρ = 1.04 for A acids, and ρ = 1.00 for benzoic acids).

Inhibitors of Histone Deacetylase

The present invention relates to hydroxamic acid derivatives that are inhibitors of histone deacetylase (HDAC). The compounds of the present invention are useful for treating cellular proliferative diseases, including cancer. Further, the compounds of the