39687-22-4

Upstream product

• 39687-20-2 (2R,3R,4S,5S,6R)-2-(benzyloxy)-6-((trityloxy)methyl)tetrahydro-2H-pyran-3,4,5-triol 
• 100-39-0 benzyl bromide 
• 77455-30-2 benzyl 6-O-triphenylmethyl-α-D-mannopyranoside 
• 100-44-7 benzyl chloride 
• 15548-45-5 (2S,3S,4S,5S,6R)-2-benzyloxy-6-(hydroxymethyl)tetrahydropyran-3,4,5-triol 
• 76-83-5 trityl chloride 
• 100-51-6 benzyl alcohol 
• 335162-25-9 benzyl α,β-D-galactopyranoside 
• 10257-28-0 D-Galactose 
• 1235200-84-6 (3R)-3-(6-O-trityl-β-D-glucopyranosyloxy)-4-pentenoic acid tert-butyl ester 
• 2280-44-6 D-Glucose 
• 54325-28-9 6-O-trityl-D-glucopyranose 
• 34246-23-6 benzyl D-glucopyranoside 
• 530-26-7 D-Mannose 

Downstream Products

• 27851-26-9 (2S,3S,4S,5R,6R)-3,4,5,6-tetrakis(benzyloxy)tetrahydro-2H-pyran-2-carboxylic acid 
• 858352-14-4 benzyl 2,3,4-tri-O-benzyl-α-D-mannopyranuronic acid 
• 120048-16-0 2,3,4-tri-O-benzyl-6-O-trityl-α-D-glucopyranose 
• 1187036-97-0 benzyl 2,3,4-tri-O-benzyl-6-O-(N-(2-ethyl-2,8-diazaspiro[4,5]decane-1,3-dione)aminocarbonyl)-β-D-glucopyranoside 

Relevant academic research and scientific papers

INHIBITORS OF MALARIAL AND PLASMODIUM FALCIPARUM HEXOSE TRANSPORTER AND USES THEREOF

Provided are molecules capable of binding to binding pockets of Plasmodium falciparum hexose transporter (PfHT) or analogs thereof and complexes comprising the same. Also provided herein are inhibitors of PfHT, pharmaceutical compositions comprising the i

Pharmaceutical composition for inhibiting tumor cell growth and application thereof

The invention discloses a pharmaceutical composition for inhibiting tumor cell growth. Its effective components include M6CP-OEt, the structural formula of M6CP-OEt is shown in the description. M6CP-OEt in the pharmaceutical composition can inhibit the gr

Glycosylated Platinum(IV) Complexes as Substrates for Glucose Transporters (GLUTs) and Organic Cation Transporters (OCTs) Exhibited Cancer Targeting and Human Serum Albumin Binding Properties for Drug Delivery

Glycosylated platinum(IV) complexes were synthesized as substrates for GLUTs and OCTs for the first time, and the cytotoxicity and detailed mechanism were determined in vitro and in vivo. Galactoside Pt(IV), glucoside Pt(IV), and mannoside Pt(IV) were highly cytotoxic and showed specific cancer-targeting properties in vitro and in vivo. Glycosylated platinum(IV) complexes 5, 6, 7, and 8 (IC50 0.24-3.97 μM) had better antitumor activity of nearly 166-fold higher than the positive controls cisplatin (1a), oxaliplatin (3a), and satraplatin (5a). The presence of a hexadecanoic chain allowed binding with human serum albumin (HSA) for drug delivery, which not only enhanced the stability of the inert platinum(IV) prodrugs but also decreased their reduction by reductants present in human whole blood. Their preferential accumulation in cancer cells compared to noncancerous cells (293T and 3T3 cells) suggested that they were potentially safe for clinical therapeutic use.

AMPHETAMINE PRODRUGS

The present invention relates to amphetamine prodrugs which provide colonic release of amphetamine.

A nonself sugar mimic of the HIV glycan shield shows enhanced antigenicity

Antibody 2G12 uniquely neutralizes a broad range of HIV-1 isolates by binding the high-mannose glycans on the HIV-1 surface glycoprotein, gp120. Antigens that resemble these natural epitopes of 2G12 would be highly desirable components for an HIV-1 vaccine. However, host-produced (self)-carbohydrate motifs have been unsuccessful so far at eliciting 2G12-like antibodies that cross-react with gp120. Based on the surprising observation that 2G12 binds nonproteinaceous monosaccharide D-fructose with higher affinity than D-mannose, we show here that a designed set of nonself, synthetic monosaccharides are potent antigens. When introduced to the terminus of the D1 arm of protein glycans recognized by 2G12, their antigenicity is significantly enhanced. Logical variation of these unnatural sugars pinpointed key modifications, and the molecular basis of this increased antigenicity was elucidated using high-resolution crystallographic analyses. Virus-like particle protein conjugates containing such nonself glycans are bound more tightly by 2G12. As immunogens they elicit higher titers of antibodies than those immunogenic conjugates containing the self D1 glycan motif. These antibodies generated from nonself immunogens also cross-react with this self motif, which is found in the glycan shield, when it is presented in a range of different conjugates and glycans. However, these antibodies did not bind this glycan motif when present on gp120.

Efficient synthesis of the functional central core lactides, a constituent of antibiotic fattiviracins

An efficient convergent synthetic method has been developed for preparation of various stereoisomers and derivatives of fattiviracins via a common lactide. The synthetic route comprises seco acids prepared by the β-selective glycosylation of chiral 3-hydroxy-4-pentanoate obtained by enzymatic kinetic resolution. The regioselective protection of four individual hydroxy groups was achieved via the 4,6-O-benzylidenation of the glucose moiety from its TMS ethers. The dimeric cyclization of the seco acids under control of reaction concentration afforded the desired lactide without using KH. Our convergent synthetic method was successfully applied to direct installation of side chains to the lactide by cross metathesis to synthesize fattiviracin derivatives. We achieved improvements to the reported method with respect to: (1) synthesis of a convergent synthetic intermediate; (2) stereoselectivity in glycosylation; and (3) establishment of a low cost route suitable for large scale synthesis.

COMPOUNDS AND COMPOSITIONS FOR THE DETECTION AND TREATMENT OF ALZHEIMER'S DISEASE AND RELATED DISORDERS

One aspect of the present invention relates to compounds, compositions and methods for diagnosis and/or treatment of a subject suffering from an amyloidosis-associated pathological condition. In certain embodiments, the imaging and/or therapeutic agents of the instant invention may be administered to a subject for identification and/or treatment of amyloid deposits. A specific imaging method detects amyloid deposits by administering the imaging agent to the subject and detecting the spatial distribution of the agent. Differential accumulation of the agent is indicative of AD or an amyIoidosis-associated pathological condition and can be monitored by using a PET or SPECT camera.

Synthesis of cyclophospho-glucoses and glucitols

The syntheses of cyclophosphodiesters of 5-C-(hydroxymethyl)-hexoses and hexitols and of 6-C-(hydroxymethyl)-hexoses are reported, along with that of 6-deoxy-gluco-heptose 7-phosphate. These compounds proved to be reasonable substrate mimics and show inhibitory activity against human d-myo-inositol 3-phosphate synthase.

METHOD AND COMPOSITION FOR SKIN DEPIGMENTATION

The present invention relates to a compound of formula I: [(C)-(L')]n-(A)-[(L)-(B)]mwherein (A) is a thioglycosylated cysteine of formula IIa or IIb: IIa IIb; (B) is a melanogenosis-inhibiting peptide comprising peptide sequence sele

Synthesis of glycosyl derivatives as dopamine prodrugs: Interaction with glucose carrier GLUT-1

Glucosyl dopamine (DA) derivatives may represent a new class of DA prodrugs that would interact with glucose transporter GLUT-1, present in the blood-brain barrier, and generate DA in the brain. Therefore, compounds bearing the sugar moiety linked to eith