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At least 397 records · Page 22Linked to original sources
PubMed2005

Recent clinical studies of the immunomodulatory drug (IMiD) lenalidomide.

Thalidomide is effective in the treatment of multiple myeloma. The immunomodulatory drug and thalidomide analogue lenalidomide is currently in late stage clinical development for MDS and multiple myeloma. This minireview highlights the course of initial and ongoing lenalidomide clinical development in oncology with reference to earlier thalidomide studies.

Clinical Trials as Topic↗
PubMed2004

Fabrication of Ni nanoparticles by selective oxidation of permalloy thin film during imidization of polyamic acid.

Ni nanoparticles embedded in a polyimide (PI) matrix were fabricated by selectively oxidizing a layer of Ni(80)Fe(20) metal film sandwiched between two PI precursor layers. Ni nanoparticles, formed in a monolayer between two PI layers, had an average particle size of approximately 5 nm. X-Ray photoelectron spectroscopy confirmed that Fe in the film was preferentially consumed, resulting in the formation of Ni nanoparticles.

Journal Article↗
PubMed2005

Glucuronidation of steroidal alcohols using iodosugar and imidate donors.

We report a study of the glucuronidation of a number of important steroidal secondary alcohols. The alcohols studied are androsterone 7, epiandrosterone 8, 17-acetoxy-androstane-3alpha,17beta-diol 9, 11alpha-hydroxyprogesterone 10, and 3-benzoylestradiol 11. These were first glucuronidated using the Schmidt trichloroacetimidate method with variations in acyl substituent (viz. derivatives 2 and 3), Lewis acid catalyst and order of addition. The results are contrasted with those obtained using our recently described glycosyl iodide donor 4, catalysed either by N-iodosuccinimide (NIS) or various metal salts.

Alcohols↗
PubMed2005

Emerging data on IMiDs in the treatment of myelodysplastic syndromes (MDS).

Myelodysplastic syndromes (MDS) encompass a spectrum of clinically diverse hematopoietic stem cell malignancies for which there are few treatment options. These disorders display remarkable heterogeneity in their hematologic and pathologic features, with a wide-ranging natural history. Complex interactions between the affected clone and the bone marrow microenvironment drive the pathogenesis and progression of MDS, resulting in ineffective hematopoiesis, blast accumulation, and a variable predisposition for progression to acute leukemia. For early stage, lower-risk patients with MDS, the mainstay of therapy is supportive care, especially red blood cell transfusions, to alleviate the symptoms of anemia. However, these interventions do not target the underlying pathobiology of disease and have questionable impact on the natural disease course. Dysregulated inflammatory, apoptotic, and angiogenic cytokines play major roles in the pathobiology of MDS and represent attractive therapeutic targets. Lenalidomide is an orally bioavailable analogue of thalidomide with more potent immunomodulatory, antiangiogenic, and antitumor activities than the parent compound and with a better safety profile. In nonclinical studies, the effects of lenalidomide include potentiation of clonogenic response to erythropoietin, activation of integrin-mediated adhesion, cell cycle arrest, sensitization to apoptotic signals, and abrogation of cellular response to receptor-initiated trophic signals. These effects have the potential to impact survival and apoptosis of erythropoietic progenitor cells and their progeny. Data from clinical trials of lenalidomide in MDS have shown erythropoietic- and cytogenetic-remitting activities that frequently result in transfusion independence, particularly in patients with 5q- deletion and lower-risk MDS. Decreases in microvessel density in bone marrow specimens from responding patients provide supportive evidence of an antiangiogenic effect in MDS. Adverse effects, most commonly myelosuppression, are generally manageable with dose reduction and growth factor support. Multicenter phase II and III studies are under way to further assess the erythroid and cytogenetic response rates in distinct subtypes of MDS, including 5q- deletion, and to optimize its clinical application.

Chromosome Aberrations↗
PubMed2004

Norfloxacin-poly(L-lysine citramide imide) conjugates and structure-dependence of the drug release.

Norfloxacin (Nflx), an antibiotic which is active against some intracellular bacteria, was coupled to a polymeric carrier, namely poly(L-lysine citramide) via a lysine or an ethylcarbamate spacer to obtain a macromolecular prodrug. The carrier, which derived from the two metabolites citric acid and L-lysine, is known to be biocompatible and slowly degradable under slight acidic conditions. Conjugates were characterised by UV, 1H and 13C NMR and SEC. The presence of Norfloxacin and the lysine type spacer caused chain aggregation, due to a probable physical cure. The release of Norfloxacin from these prodrugs and from a prodrug where Norfloxacin is bound to the carrier backbone without spacer arm was investigated comparatively in vitro. Conjugation via a carbamate-type linkage appeared as a method to achieve the release of Norfloxacin from a PLCA-type conjugate at neutral.

Drug Carriers↗
PubMed1998

Uptake and intracellular distribution of 4-aminofluorescin-labelled poly(L-lysine citramide imide) in K562 cells.

4-Aminofluorescein (F1-NH2) was conjugated with various macromolecular carriers of the poly(L-lysine citramide)-type which were hydrophobised by ethyl (C2), heptyl (C7), and dodecyl (C12) alkyl groups attached to the pendent carboxyl of the lysine moieties present in repeating units. The dye was used to label the carriers and monitor their intracellular fate after introduction within the incubation medium of K562 cells. The labelled hydrophobised carriers formed multimolecular compacted aggregates stabilised by the balance of attractive hydrophobic interactions and repulsive electrostatic forces in the aqueous culture medium. The apparent molecular weights and the sizes of these aggregates were determined by Size Exclusion Chromatography (SEC) and by light scattering respectively. Comparison was made of the cell distribution of free and conjugated F1-NH2 in the cell cytoplasm and nucleus by using fluorescence microscopy and laser microspectrofluorometry. It was shown that cell uptakes resulted from adsorptive pinocytosis and depended on hydrophobicity and aggregation of the conjugates. The influence of physical entrapment of free-F1-NH2 within the hydrophobic microdomains formed by aggregates F1-NH2 conjugates was also discussed.

Chromatography, Gel↗
PubMed1999

Novel small molecule nonpeptide aminopeptidase n inhibitors with a cyclic imide skeleton.

A novel series of small molecule nonpeptide aminopeptidase N (APN) inhibitors with a N-phenylphthalimide or N-phenylhomophthalimide skeleton were prepared. Evaluation of their protease inhibitory activities revealed that (i) some N-phenylphthalimide analogs are potent APN inhibitors, but they are also inhibitors of another protease, dipeptidylpeptidase IV (DPP-IV), and (ii) some N-phenylhomophthalimide analogs, including 2-(2,6-diethylphenyl)-1,2,3,4-tetrahydroisoquinoline-1,3-dione (PIQ-22), are potent and specific inhibitors of APN without DPP-IV-inhibitory activity. The structure-activity relationship studies of N-phenylphthalimides and N-phenylhomophthalimides are reviewed. PIQ-22 showed potent tumor-cell invasion-inhibitory activity.

Antineoplastic Agents↗
PubMed1986

Pyridyl groups for protection of the imide functions of uridine and guanosine. Exploration of their displacement reactions for site-specific modifications of uracil and guanine bases.

For the protection of the O-4 function of uridine and the O-6 of guanosine, 2-, 3- and 4-hydroxypyridines, 2-pyridinethiol, 6-methyl-2-hydroxy- and 6-methyl-3-hydroxypyridines have been employed. These substituted pyridines gave pyridyl-N-and/or pyridyl-O-substituted derivatives, depending both upon the position of the hydroxyl and methyl groups in the pyridine ring, at the C-4 and the C-6 of the uracil and guanine residues, respectively. These groups were found to be good leaving groups for nucleophilic substitution reactions by amines, thiolates and oximate. If needed, the rate of these substitution reactions could be conveniently increased by almost 1000-fold by conversion of the pyridyl moiety to its methiodide.

Chemical Phenomena↗