An hydroformylation-based approach to the synthesis of the odorant Florhydral® has been investigated. The hydroformylation of m-diisopropenylbenzene (2) in the presence of rhodium catalysts leads to mixtures of 3-(3-isopropenylphenyl)butyraldehyde (3), which is an immediate precursor of Florhydr...
An efficient total synthesis of (+)-sporogen-AO 1 (13-desoxyphomenone) 1 was achieved in 20 steps from ethyl (1R,2S)-5,5-ethylenedioxy-2-hydroxycyclohexane-carboxylate 3 in 8.3% overall yield. The optically active 3 with 98.4% e.e. was easily obtained in 74% yield by the reduction of the corresp...
In order to design and develop potential anticancer drugs involving the same structural pattern as platinum(II) antitumor complexes, complexes of palladium and platinum with 3-methyl-orotic acid as the leaving ligand have been synthesized. The study of the anticancer activity of these compounds ...
The novel dual targeted nanoparticles loaded with doxorubicin (DOX) and magnetic nanoparticles (MNPs) were prepared for treatment of breast cancer. Nanoparticles were produced by a layer-by-layer technique and functionalized with a bioconjugate of chitosan-poly(methyl vinyl ether maleic acid)(PM...
LHRH based vaccines are promising candidates for therapy of androgen and estrogen dependent cancers. We report in this communication development of a novel recombinant protein vaccine candidate against LHRH. A synthetic gene was designed in which the codon sequence in the LHRH decapeptide was mo...
The rapid and simple detection of circulating tumor cells (CTCs) can enable early diagnosis and improve prognosis in cancer patients. Here, we fabricated luteinizing hormone releasing hormone (LHRH)-conjugated surface-enhanced Raman scattering (SERS) tags to detect CTCs expressing LHRH receptors...
Targeted therapy is an emerging technique in cancer detection and treatment. This paper presents the results of a combined experimental and theoretical study of the specific targeting and entry of luteinizing hormone releasing hormone (LHRH)-conjugated PEG-coated magnetite nanoparticles into tri...
Ethnopharmacological relevanceCimicifuga racemose is previously proved effective on nature menopausal syndrome (MPS). However, its clinical value in treating with MPS induced by luteinizing-hormone releasing hormone analogue (LHRH-a) therapy of pre-/peri-menopausal breast cancer patients is stil...
Genetic algorithm combined with density functional theory has been used to study (CuF)n (n = 1–12) clusters. The clusters are optimized by TPSSh/Lanl2dz (Cu)/6-31G(d) (F) method. Benchmark calculations have been carried out to find out suitable method and basis sets to calculate energies. The r...
First principles studies on the electronic structure, stability, and magnetic properties of CrnTem (1 ≤ n ≤ 6, 1 ≤ m ≤ 8) clusters have been carried out within a density functional framework. Investigations into the energetic stability indicate that Cr4Te6 and Cr6Te8 are energetically stable...
Condensation of 6-O-benzyl-7,8-dideoxy-1,2:3,4-di-O-isopropylidene-d-glycero-α-d-galacto-oct-7-ynopyranose with methyl 2,3,4-tri-O-benzyl-6-deoxy-β-d-galacto-heptodialdo-1,5-pyranoside afforded a 2:1 mixture of the 1S and 1R isomers (1a and 1b) of 3-[6(R)-O-benzyl-1,2:3,4-di-O-isopropylidene-α...
Demand for lactic acid is growing, especially, for its use in the production of biodegradable polymer (polylactate). The current method of production and separation of lactic acid is both expensive and unsustainable. This is partly due to the cost and lower efficiency of the current method for s...
Polycyclic 1,4-dihydrobenzothieno[3,2-b]pyridine 5,5-dioxides and 4,5-dihydro-1H-indeno[1,2-b]pyridines having ester or cyano group at the position 3 of dihydropyridine ring have been synthesised. Reactivity of N-bromosuccinimide (NBS) towards polycyclic 1,4-dihydropyridine derivatives has been ...
A series of novel trifluoromethyl substituted furo[2,3-b]pyridine and pyrido[3′,2′:4,5]furo[3,2-d] pyrimidine derivatives 3a-b, 6a-k, 9, 10a-b, 11a-c and 12a-c were prepared from 2-carbethoxy-3-amino-6-trifluoromethyl furo[2,3-b]pyridine 1 under different set of conditions. Compounds functiona...
Four sulfanilamide derivatives N-[4-(phenylsulfamoyl)phenyl]acetamide (1), 4-amino-N-phenylbenzenesulfonamide (2), N-[4-(phenylsulfamoyl)phenyl]benzamide (3) and N-{4-[(3-chlorophenyl)sulfamoyl]phenylbenzamide (4) were synthesized and characterized by Infra-Red (IR), Nuclear Magnetic Resonance (...
A series of 3-unsubstituted/substituted-4,5-diphenyl-2-oxo-3H-1,3-oxazole derivatives were prepared as selective cyclooxygenase-2 (COX-2) inhibitors. Among the synthesized compounds, 4-(4-phenyl-3-methyl-2-oxo-3H-1,3-oxazol-5-yl)benzensulfonamide (compound 6) showed selective COX-2 inhibition wi...
The use of a two-level heterobifunctional agent N-(m-aminobenzoyloxy)succinimide (m-ABS) allowed us to develop a new method for preparing hapten-protein conjugates. This was demonstrated by a conjugation between thyrotropin-releasing hormone (TRH) and bovine or human serum albumin (BSA or HSA). ...
Three geometric ortho-, meta-, and para-isomers of N-(aminobenzoyloxy)succinimide (ABS) were synthesized, and their usefulness as a two-level heterobifunctional cross-linking agent in the preparation of hapten-protein conjugates was evaluated. The conjugation was based on the principle that ABS ...
Based on their mol. wts, notexin and scutoxin elute later than expected from gel filtration columns in multiple peaks [Francis et al. (1991) Toxicon29, 85–96]. Notexins present in these peaks have identical amino acid sequences and unmodified amino acid side-chains. Scutoxin is an isoform of no...
Background: Two deoxysugar glycosyltransferases (GTs), UrdGT1b and UrdGT1c, involved in urdamycin biosynthesis share 91% identical amino acids. However, the two GTs show different specificities for both nucleotide sugar and acceptor substrate. Generally, it is proposed that GTs are two-domain pr...
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