16446-73-4

Upstream product

• 6304-89-8 3-acetoxybenzoic acid 
• 99-06-9 3-Carboxyphenol 
• 108-39-4 3-methyl-phenol 
• 122-46-3 3-acetoxytoluene 

Downstream Products

• 88-15-3 2-Acetylthiophene 
• 106882-29-5 (3-acetoxy-phenyl)-[2]thienyl ketone 
• 4265-18-3 3-acetyl-2-ethylbenzofuran 
• 109615-04-5 (3-acetoxy-phenyl)-(2-ethyl-benzofuran-3-yl)-ketone 
• 111297-22-4 4-(3-acetoxy-benzoyloxy)-coumarin 
• 108897-14-9 3-acetoxy-4'-methoxy-benzophenone 
• 100-06-1 1-(4-methoxyphenyl)ethanone 
• 1020171-55-4 3-(3-acetoxy-benzoyloxy)-benzoic acid 
• 15789-04-5 N,N-diethyl-3-hydroxybenzamide 
• 109251-36-7 3'-acetoxy-2,4-dimethoxy-benzophenone 
• 79-20-9 acetic acid methyl ester 
• 19438-10-9 methyl 3-hydroxybenzoate 
• 38031-61-7 1-(5-isopropyl-4-methoxy-2-methyl-phenyl)-ethanone 
• 112116-42-4 3'-acetoxy-5-isopropyl-4-methoxy-2-methyl-benzophenone 

Relevant academic research and scientific papers

Evaluation of N-Hydroxy-, N-Metoxy-, and N-Acetoxybenzoyl-Substituted Derivatives of Thymine and Uracil as New Substances for Prevention and Treatment of Long-Term Complications of Diabetes Mellitus

New uracil and thymine derivatives, N1-,N3- and N1,N3-(RO-benzoyl)-(1H,3H)-pyrimidine- 2,4-diones, were synthesized (RO- is hydroxy, acetoxy- or methoxy-group). The compounds were studied in a complex of in vitro tests for the ability to inhibit the development of long-term complications of diabetes. Their ability to cleave cross-links of proteins has been evaluated. The most significant ways of pharmacological correction of thrombosis, angio-, nephro-, encephalo-, and cardiopathy, antiglycation, chelating, and antiplatelet activities, have been established. The most active compound in terms of antiplatelet action, N1- hydroxybenzoyluracil, exceeded acetylsalicylic acid by ~44%. In terms of their ability to chelate copper (II) cations, all compounds (with the exception of 1,3-bis(3-hydroxybenzoyl)-(1H,3H)-pyrimidine-2,4-dione that was not not studied in this test) showed the activity, whose IC50 fell in the range between that for pioglitazone (44.1 μM) and pyridoxamine (136.7 μM) comparison drugs. The best antiglycation effect at the 1 mM concentration was observed for N1,N3-bismethoxy- and N1,N3-bisacetoxybenzoyl derivatives of thymine. The maximum activity to cleave cross-links of proteins (C = 1 mM), comparable to that of alagebrium, was established for 1,3-bis(4-methoxybenzoyl)uracil, for which also high rates of other estimated activities were noted. Thus, the N1-,N3- and N1,N3-(RO-benzoyl) derivatives of uracil and thymine are promising basiсs for creating drugs that suppress the development of long-term complications of diabetes.

Structure-Activity Study of Nitazoxanide Derivatives as Novel STAT3 Pathway Inhibitors

We identified nitazoxanide (NTZ) as a moderate STAT3 pathway inhibitor through immunoblot analysis and a cell-based IL-6/JAK/STAT3 pathway activation assay. A series of thiazolide derivatives were designed and synthesized to further validate the thiazolide scaffold as STAT3 inhibitors. Eight out of 25 derivatives displayed potencies greater than that of NTZ, and their STAT3 pathway inhibitory activities were found to be significantly correlated with their antiproliferative activities in HeLa cells. Derivatives 15 and 24 were observed to be more potent than the positive control WP1066, which is under phase I clinical trials. Compared with NTZ, 15 also exhibited much improved in vivo pharmacokinetic parameters in rats and efficacies against proliferations in multiple cancer cell lines, indicating a broad-spectrum effect of these thiazolides as antitumor agents targeted on STAT3.

Hydroxybenzoyl Chlorides in the Synthesis of Conjugates with Biologically Active Dipeptides

Abstract: Conjugates of hydroxy- and acetoxybenzoic acids with dipeptides based on 4-aminobutanoic acid and glycine were synthesized through hydroxy(acetoxy)benzoyl chlorides and 4-[hydroxy(acetoxy)benzoyl-amino]butanoyl chlorides as intermediate products. Acyl chlorides were prepared by treatment of the corre-sponding acids with oxalyl chloride in the presence of dimethylformamide at a ratio of 1:1.1:0.07 in boiling benzene. The target N-[hydroxy(acetoxy)benzoyl] derivatives of dipeptides were obtained with high yields, and no further purification of the products was necessary. The synthesized compounds were evaluated as potential neuroprotective agents.

Discovery of 4-methyl-N-(4-((4-methylpiperazin- 1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((6-(pyridin-3-yl)-1H-pyrazolo[3,4-d]pyrimidin-4-yl)-oxy)benzamide as a potent inhibitor of RET and its gatekeeper mutant

The receptor tyrosine kinase rearranged during transfection (RET) plays pivotal roles in several cancers, including thyroid carcinoma and non-small cell lung cancer (NSCLC). Currently, there are several FDA-approved RET inhibitors, but their indication is limited to thyroid cancer, and none can overcome their gatekeeper mutants (V804L and V804M). Here, we report the discovery of 9x representing a new chemotype of potent and selective RET inhibitors, using a rational design strategy of type II kinase inhibitors. 9x exhibited both superior antiproliferative activities against NSCLC-related carcinogenic fusions KIF5B-RET and CCDC6-RET and gatekeeper mutant-transformed Ba/F3 cells, with the lowest GI50 of 9 nM, and substantial inhibitory activities against wild-type RET and RET mutant proteins, with the best IC50 of 4 nM. More importantly, 9x also showed nanomole potency against RET-positive NSCLC cells LC-2/ad, but not against a panel of RET-negative cancer cells, such as A549, H3122, A375 or parental Ba/F3 cells, demonstrating its selective ‘on-target’ effect. In mouse xenograft models, 9x repressed tumor growth driven by both wild type KIF5B-RET-Ba/F3 and gatekeeper mutant KIF5B-RET(V804M)-Ba/F3 cells in a dose-dependent manner. Together, these data establish that 9x provides a good starting point for the development of targeted therapeutics against RET-positive cancers, especially NSCLC.

SMALL MOLECULE MODULATORS OF THE ANDROGEN RECEPTOR

Provided herein are compounds useful for modulating the activity of an androgen receptor, or a variant thereof, and related compositions and methods. Compounds of the invention are useful for antagonizing the androgen receptor splice variant AR-v7, and fo

Uracil Hydroxybenzamides as Potential Antidiabetic Prodrugs

A series of N1, N3-bis-hydroxybenzoyl, -acetoxybenzoyl, and -methoxybenzoyl uracil derivatives were synthesized. All compounds were screened for the ability to rupture protein cross links and antiglycating, chelating, and antiaggregant properties, which are most significant for pharmacological treatment of thrombosis and angio-, nephro-, encephalo-, and cardiopathies. 1,3-bis-(4-Methoxybenzoyl)pyrimidine-2,4(1H,3H)-dione was a promising antidiabetic agent with all studied activities.

(Phosphinito)aryl benzimidazole PCN pincer palladium(II) complexes: Synthesis, characterization and catalytic activity in C–H arylation of azoles with aryl iodides

The PCN pincer Pd(II) complexes 4a–c with (phosphinito)aryl benzimidazole ligands were conveniently synthesized by one-pot phosphorylation/palladation reaction of a (2-benzimidazolyl)-containing m-phenol derivative 3. The three complexes were well characterized by spectroscopic methods, elemental analysis and their molecular structures were further determined by X-ray single-crystal diffraction. The Pd(II) center in each complex adopts a typical distorted-square-planar geometry. With a catalyst loading of 0.25–0.5 mol%, complex 4a could effectively catalyze C–H arylation of benzothiazole, benzoxazole and thiazole with various aryl iodides in the presence of CuI as a cocatalyst.

Technological method for preparing m-aminophenol

The invention relates to a technological method for preparing m-aminophenol, belongs to the technical field of chemical material preparation and solves the technical problem of limit caused by utilizing phenyl acetate as a preparation raw material. The technological method disclosed by the invention has the advantages of simpleness in operation, high product yield, reaction easy to control and thelike. The technological method is characterized by comprising the steps: preparing 3-carboxyphenyl phenyl acetate after preparing m-cresyl acetate and utilizing the prepared 3-carboxyphenyl phenyl acetate to prepare the m-aminophenol. The technological method comprises the steps: a, taking a C9H8O4 solvent, adding into an ethyl acetate solution, fully stirring until complete dissolution, dropwiseadding thionyl chloride into a system under the ice water bath condition, thermally insulating 1+/-0.5 hours, warming to 60 DEG C and refluxing; b, under the ice water bath condition, adding triethylamine and hydroxylamine hydrochloride into the system, thermally insulating for 2 hours and warming to a room temperature; c, spin drying the solvent on a rotary evaporator, then adding water and potassium carbonate, warming to 60 to 70 DEG C and hydrolyzing; d, utilizing ethyl acetate to extract the solution, utilizing a thin-layer chromatography to determine whether extraction is complete and obtaining the finished product of the m-aminophenol after the extraction is finished.

Synthesis and anticancer activity evaluation of some new derivatives of 2-(4-benzoyl-1-piperazinyl)-quinoline and 2-(4-cinnamoyl-1-piperazinyl)-quinoline

In this study, we designed and synthesized twenty new derivatives of 2-(4-benzoyl-1-piperazinyl)- quinoline and 2-(4-cinnamoyl-1-piperazinyl)-quinoline with potential anticancer activity. The structures of synthesized compounds were confirmed by 1H and 13C NMR spectroscopy and MS spectrometry. The activity of novel compounds was evaluated in the cell viability assay as well as in the wound healing assay. Presented data show that examined substances have anticancer activity in cell culture. Seven compounds which showed a high rate of cell growth inhibition were selected for further studies. Three of them strongly reduced the growth of B16F10 cells. The novel compounds constitute a good base for further studies and optimization of structure for new therapeutically effective anti-cancerous drugs.

(R)- AND (S)-1-(3-(3-N,N-DIMETHYLAMINOCARBONYL)PHENOXYL-4-NITROPHENYL)-1-ETHYL-N,N'-BIS (ETHYLENE)PHOSPHORAMIDATE, COMPOSITIONS AND METHODS FOR THEIR USE AND PREPARATION

Provided herein are optically active compounds of the formulae (ii); and (III) and pharmaceutical compositions thereof. Also provided herein are processes of making these compounds and resolving the racemic mixture or the enrichment of same with in one of