90512-18-8

Upstream product

• 350-46-9 4-Fluoronitrobenzene 
• 111-46-6 diethylene glycol 
• 100-02-7 4-nitro-phenol 
• 628-89-7 2-(2-Chloroethoxy)ethanol 
• 118591-58-5 5-tosyloxy-3-oxapentanol 
• 100-00-5 4-chlorobenzonitrile 

Relevant academic research and scientific papers

Di-substituted maleic amide linker for antibody drug conjugating and preparation method and use thereof

Provided in the present invention are a di-substituted maleic amide linker conjugated to an antibody and a preparation method and use thereof. In particular, the present invention conjugates a strongly cytotoxic active substance to a biomacromolecule thro

Flexible multidentate benzyldiamine derivatives with high affinity for β-amyloid in cerebral amyloid angiopathy

Abstract: Cerebral amyloid angiopathy (CAA) commonly found in the aged is pathologically characterized by β-amyloid (Aβ) deposition in the walls of arteries and capillaries of brain. In this study, four flexible multidentate benzyldiamine derivatives as potential probes for cerebrovascular Aβ deposition were designed and synthesized. In in vitro inhibition assays, the ligands 18–21 displayed high affinities for Aβ aggregates with Ki values of 1.45 ± 0.53?nM, 1.68 ± 0.35?nM, 1.16 ± 0.23?nM and 1.72 ± 0.19?nM, respectively. A significant improvement in the binding affinity over the monomer, compounds 9–12 or benzyldiamine derivatives, demonstrated the applicability of the multidentate approach. The underlying mechanism of these novel Aβ agents was explored by molecular docking technique, which theoretically verified the high affinities of the multidentate benzyldiamine derivatives for Aβ aggregates. Moreover, the molecular masses of the ligands 18–21 are more than 700 Dalton, which are believed to be hardly capable of penetrating blood brain barrier. In this regard, these ligands could be used to distinguish CAA from Alzheimer’s disease which is another Aβ-related disorder disease. To convert these ligands to positron emission tomography imaging agents, we attempted to radiosynthesize [18F]18. Though the radiolabeling was not very successful, the preliminary results suggested that these newly proposed multidentate benzyldiamine derivatives may be used as potential Aβ imaging agents in cerebral amyloid angiopathy. Graphic abstract: [Figure not available: see fulltext.].

Discovery of Diphenoxy Derivatives with Flexible Linkers as Ligands for β-Amyloid Plaques

The highly rigid and planar scaffolds with π-conjugated systems have been widely considered to be indispensable for β-amyloid (Aβ) binding ligands. In this study, a library of diphenoxy compounds with different types of more flexible linkers as Aβ ligands were synthesized and evaluated. Most of them displayed good affinity (Ki1-42aggregates, and some ligands even showed values of Kiless than 10 nM. Structure-activity relationship analysis revealed that modification on the linkers or substituents tolerated great flexibility, which challenged the long-held belief that rigid and planar structures are exclusively favored for Aβ binding. Three ligands were labeled by iodine-125, and they exhibited good properties in vitro and in vivo, which further supported that this flexible scaffold was potential and promising for the development of Aβ imaging agents.

Glycosylated tris-bipyridine ferrous complexes for probing a mechanism behind carbohydrate-carbohydrate interactions: Spatial carbohydrate packing of glycoclusters changes on additions of salts in carbohydrate- and anion-dependent manners

2,2′-Bipyridines containing two β-maltoside, β-lactoside, or β-isomaltoside appendages were prepared and successively complexed with ferrous ion to afford hexavalent glycoclusters having tris-bipyridine ferrous complex cores. Each of these metalloglycoclu

Synthesis and evaluation of novel F-18-labeled pyrimidine derivatives: Potential FAK inhibitors and PET imaging agents for cancer detection

Based on computer-assisted drug design, a series of novel pyrimidine derivatives was successfully synthesized and characterized by 1H NMR, 13C HNMR, and MS spectra. All the new compounds were evaluated for their activity against focal adhesion kinase and showed low IC50 values in comparison with control drugs. In particular, for compound 8i, its IC50 value was 0.060 μM, suggesting its advantage as a focal adhesion kinase inhibitor. To evaluate the potentiality of these compounds as PET imaging agents in cancer detection, compounds 8a, 8c, 8h, and 8i were successively labeled with 18F. The four 18F-labeled pyrimidine derivatives showed appropriate log P values and high stability in physiological saline and mouse plasma. Noticeably, compound [18F]-8a with a 4-methoxyl group at the benzene ring exhibited good in vivo biodistribution data in mice bearing the S180 tumor, which promoted a further microPET imaging study of compound [18F]-8a. The microPET image of [18F-8a] administered into the S180 tumor-bearing mice acquired at 60 min post-injection illustrated that the uptake in S180 tumor was obvious. These results suggested that compound [18F]-8a might be a new probe for PET tumor imaging.

Diphenoxyl flexible molecules with high affinity with A[beta] plaque and preparation method and applications thereof

The invention discloses diphenoxyl flexible molecules with high affinity with A[beta] plaque and a preparation method and applications thereof. After the molecules are labeled by radionuclide, the molecules can be used as an A[beta] plaque developing agen

NOVEL AROMATIC COMPOUND AND USE THEREOF

Provided is a compound showing a bone formation promoting action (and/or bone resorption suppressive action). A compound of the formula (I) or a pharmacologically acceptable salt: [wherein each substituent is as defined in the DESCRIPTION], has low toxicity, shows good pharmacokinetics, has an action to promote bone formation, and is useful for the prophylaxis or To treatment of metabolic bone diseases (osteoporosis, fibrous osteitis (hyperparathyroidism), osteomalacia, Paget's disease that influences the systemic bone metabolism parameter etc.) associated with a decrease in the bone formation ability as compared to the bone resorption capacity.

Alkoxylation of 4-chloronitrobenzene with aliphatic alcohols and glycols in the presence of NaOH

The reaction of 4-chloronitrobenzene with aliphatic C1-n-C 4 alcohols and with mono-, di-, and triethylene glycols in the presence of NaOH in liquid ammonia at 15-50°C was studied.