89950-93-6

Upstream product

• 2417-72-3 Methyl 4-(bromomethyl)benzoate 
• 6232-88-8 4-bromomethylbenzoic Acid 
• 75-16-1 methylmagnesium bromide 
• 153813-69-5 methyl 4-formyl-3-nitrobenzoate 
• 55737-66-1 2-nitro-4-methoxycarbonylbenzoic acid 
• 55715-03-2 4-bromomethyl-3-nitrobenzoic acid 
• 88089-94-5 methyl 4-bromomethyl-3-nitrobenzoate 
• 142386-70-7 methyl 4-acetoxymethyl-3-nitrobenzoate 
• 67-56-1 methanol 
• 82379-38-2 4-(hydroxymethyl)-3-nitrobenzoic acid 

Downstream Products

• 89950-94-7 4-methoxycarbonyl-2-nitrobenzyl-2,3,4,6-tetra-O-acetyl-β-D-glucopyranoside 
• 51885-90-6 methyl 4-(chloromethyl)-3- nitrobenzoate 
• 142386-72-9 4-carboxy-2-nitrobenzyl O-α-D-glucopyranosyl-(1->6)-O-α-D-glucopyranosyl-(1->4)-β-D-glucopyranoside 
• 104932-53-8 4-carboxy-2-nitrobenzyl O-α-D-glucopyranosyl-(1->4)-O-α-D-glucopyranosyl-(1->4)-β-D-glucopyranoside 
• 126412-67-7 4-methoxycarbonyl-2-nitrobenzyl 2,3-di-O-acetyl-4,6-di-O-(3,4,6-tri-O-acetyl-α-D-glucopyranosyl)-β-D-glucopyranoside 
• 126412-66-6 4-methoxycarbonyl-2-nitrobenzyl 2,3-di-O-acetyl-4-O-(2,4,6-tri-O-acetyl-α-D-glucopyranosyl)-β-D-glucopyranoside 
• 142386-73-0 C₂₇H₃₉NO₂₀ 
• 126412-68-8 4-carboxy-2-nitrobenzyl 4,6-di-O-α-D-glucopyranosyl-β-D-glucopyranoside 
• 126412-64-4 4-methoxycarbonyl-2-nitrobenzyl 2,3-di-O-acetyl-4,6-O-<1,1,3,3-tetra(2-propyl)-disiloxan-1,3-yl>-β-D-glucopyranoside 
• 126412-65-5 4-methoxycarbonyl-2-nitrobenzyl 2,3-di-O-acetyl-β-D-glucopyranoside 
• 126412-63-3 4-methoxycarbonyl-2-nitrobenzyl β-D-glucopyranoside 

Relevant academic research and scientific papers

PRODRUG-TYPE ANTICANCER AGENT USING CANCER-SPECIFIC ENZYMATIC ACTIVITY

To provide novel compounds that are promising as prodrug-type anticancer agents, a compound represented by general formula (I) or a salt thereof is provided.

Investigations into the potential role of metabolites on the anti-leukemic activity of imatinib, nilotinib and midostaurin

The efficacy and side-effects of drugs do not just reflect the biochemical and pharmacodynamic properties of the parent compound, but often comprise of cooperative effects between the properties of the parent and active metabolites. Metabolites of imatinib, nilotinib and midostaurin have been synthesised and evaluated in assays to compare their properties as protein kinase inhibitors with the parent drugs. The N-desmethylmetabolite of imatinib is substantially less active than imatinib as a BCR-ABL1 kinase inhibitor, thus providing an explanation as to why patients producing high levels of this metabolite show a relatively low response rate in chronic myeloid leukaemia (CML) treatment. The hydroxymethylphenyl and N-oxide metabolites of imatinib and nilotinib are only weakly active as BCR-ABL1 inhibitors and are unlikely to play a role in the efficacy of either drug in CML. The 3-(R)-HO-metabolite of midostaurin shows appreciable accumulation following chronic drug administration and, in addition to mutant forms of FLT3, potently inhibits the PDPK1 and VEGFR2 kinases (IC50 values 100 nM), suggesting that it might contribute to drug efficacy in acute myeloid leukaemia patients. The case studies discussed here provide further examples of how the synthesis and characterisation of metabolites can make important contributions to understanding the clinical efficacy of drugs.

Structure-Based Drug Design of Potent Pyrazole Derivatives against Rhinovirus Replication

Rhinoviruses (RVs) have been linked to exacerbations of many pulmonary diseases, thus increasing morbidity and/or mortality in subjects at risk. Unfortunately, the wide variety of RV genotypes constitutes a major hindrance for the development of Rhinovirus replication inhibitors. In the current investigation, we have developed a novel series of pyrazole derivatives that potently inhibit the Rhinovirus replication. Compounds 10e and 10h behave as early stage inhibitors of Rhinovirus infection with a broad-spectrum activity against RV-A and RV-B species (EC50 0.1 μM). We also evaluate the dynamics of the emerging resistance of these promising compounds and their in vitro genotoxicity. Molecular docking experiments shed light on the pharmacophoric elements interacting with residues of the drug-binding pocket.

[6,6] FUSED BICYCLIC HDAC8 INHIBITORS

The present invention is directed to compounds of Formula I: and pharmaceutically acceptable salts, prodrugs, solvates, hydrates, tautomers, or isomers or thereof, wherein R1, R2, R2', L, X, W, Y1,Y2,

Solid-phase synthesis and hybrization behavior of partially 2′/3′-O-acetylated RNA oligonucleotides

Synthesis of partially 2′/3′-O-acetylated oligoribonucleotides has been accomplished by using a 2′/3′-O-acetyl orthogonal protecting group strategy in which non-nucleophilic strong-base (DBU) labile nucleobase protecting groups and a UV-light cleavable linker were used. Strong-base stability of the photolabile linker allowed on-column nucleobase and phosphate deprotection, followed by a mild cleavage of the acetylated oligonucleotides from the solid support with UV light. Two 17nt oligonucleotides, which were synthesized possessing one specific internal 2′- or 3′-acetyl group, were used as synthetic standards in a recent report from this laboratory detailing the prebiotically plausible ligation of RNA oligonucleotides. In order to further investigate the effect of 2′/3′-O-acetyl groups on the stability of RNA duplex structure, two complementary bis-acetylated RNA oligonucleotides were also expediently obtained with the newly developed protocols. UV melting curves of 2′-O-acetylated RNA duplexes showed a consistent ～3.1 °C decrease in Tm per 2′-O-acetyl group.

Disaccharide synthesis on a soluble hyperbranched polymer

A hyperbranched star polymer was employed as a soluble support for disaccharide synthesis as a practical alternative to a dendrimer support. The large number of terminal groups present on the support permit very high loading levels to be possible. Polymer bound intermediates could be directly analyzed by MALDI-TOF mass spectrometry due to the presence of a photolabile linker that is cleaved by the MALDI-TOF laser.

Radical and palladium-mediated cyclizations of ortho-iodo benzyl enamines: A scope and limitation study

Radical and palladium-mediated cyclizations of ortho-iodo benzyl enamines were compared to determine their potential application to the synthesis of libraries of compounds on solid support.

Combinatorial dihydrobenzopyran library

Combinatorial libraries are disclosed which are represented by Formula I: wherein: S is a solid support; T'--L-- is an identifier residue; and --L'--II' is a ligand/linker residue. These libraries contain dihydrobenzopyrans of the formula: STR1 which interact (i.e., as agonists or antagonists) with α adrenergic receptors, dopamine receptors, ?-opiate receptors, and K+ channels and are inhibitors of carbonic anhydrase isozymes. They are useful in the treatment of ocular diseases such as glaucoma.

PROCESS FOR PREPARING INTERMEDIATES FOR A COMBINATORIAL DIHYDROBENZOPYRAN LIBRARY

Combinatorial libraries are disclosed which are represented by Formula I:(T'-L) q-S-C(O)-L'-II' I wherein:S is a solid support; T'-L-is an identifier residue; and-L'-II' is a ligand/linker residue. These libraries contain dihydrobenzopy