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Prodrugs (0):
Recent article
Prodrugs
Abstract
We identify a previously unknown target of POA as the ribosomal protein S1 (RpsA), a vital protein involved in protein translation and the ribosome-sparing process of trans-translation. Three PZA-resistant clinical isolates without pncA mutation harbored RpsA mutations. RpsA overexpression conferred...
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PMID: 21835980
PDF is available here.
PDF is available here.
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Abstract
We treat disorders such as rheumatoid arthritis (RA), as well as a range of other inflammatory diseases. Fostamatinib (R-788) is an orally bioavailable small molecule. It is the prodrug of R406, which is a potent Syk inhibitor. Fostamatinib was developed because it has more favourable physiochemical...
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PMID: 21711059
PDF is available here.
PDF is available here.
Arthritis & Rheumatism (63)2 2011
Abstract
Our findings indicate that there were no differences in the primary end point between the R788 and placebo groups. Differences were observed between the R788 and placebo groups in secondary end points, particularly in those patients who entered the study with an elevated CRP level.
C...
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PMID: 21279990
PDF is available here.
PDF is available here.
Immunotherapy (3)2 2011
Abstract
Advances in biomolecular technology have allowed the development of genetically fused antibody-enzymes. Antibody-enzyme fusion proteins have been used to target tumors for cancer therapy in two ways. In one system, an antibody-enzyme is pretargeted to the tumor followed by administra...
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PMID: 21322759
PDF is available here.
PDF is available here.
Abstract
We determined the pharmacokinetics of mycophenolic acid (MPA) and its metabolites mycophenolic acid glucuronide (MPAG) and acyl glucuronide (AcMPAG) in rat plasma and bile, using a newly developed HPLC method. Protein precipitation and liquid-liquid extraction were employed in sample preparation of...
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PMID: 21468916
PDF is available here.
PDF is available here.
Abstract
The FDA has approved the oral direct thrombin inhibitor dabigatran (da big' a tran) etexilate (Pradaxa--Boehringer Ingelheim) for prevention of thromboembolic stroke in patients with non-valvular atrial fibrillation.It has been available in Canada (Pradax) since 2008 for prevention of thromboembolis...
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PMID: 21068702
PDF is available here.
PDF is available here.
Abstract
The administration of dual antiplatelet therapy with aspirin and a thienopyridine for the prevention of thrombosis in patients with acute coronary syndrome undergoing percutaneous coronary intervention is proven to reduce mortality. The original thienopyridine, ticlopidine, has largely been displace...
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PMID: 20839914
PDF is available here.
PDF is available here.
Cancer Treatment Reviews (36 Suppl 3) 2010
Abstract
Capecitabine is an orally administered fluoropyrimidine carbamate which has been developed as a prodrug of 5-FU with the goal to improve its tolerability and intratumoral drug concentration. The review aims to provide an evidence-based update of clinical trials investigating the clinical efficacy, a...
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PMID: 21129610
PDF is available here.
PDF is available here.
Abstract
We were interested to see if we could use PfTMPK to activate 3'-azido-2',3'-deoxythymidine (AZT) derivatives as a strategy to treat malaria. P. falciparum lacks a pyrimidine nucleoside kinase which usually activates nucleoside and nucleoside analogues to the corresponding monophosphates. Therefore,...
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PMID: 20833052
PDF is available here.
PDF is available here.
Abstract
Density Functional Theory (DFT) and ab initio calculation results for the proton transfer reaction in Kirby's enzyme models 1-6 reveal that the reaction rate is largely dependent on the existence of a hydrogen bonding net in the reactants and the corresponding transition states. Further, the distanc...
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PMID: 20731669
PDF is available here.
PDF is available here.
Abstract
Chemotherapy induced nausea and vomiting (CINV) is a common complication in the treatment of patients with cancer. The introduction of the first in class neurokinin-1 receptor antagonist aprepitant provided additive control on CINV in combination to existing antiemetics. Due to formulation issues, ap...
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PMID: 20795794
PDF is available here.
PDF is available here.
Abstract
A one-pot route to 8-substituted xanthines has been developed from 5,6-diaminouracils and carboxaldehydes. Yields are good and the process applicable to a range of substrates including a family of A(2A) adenosine receptor antagonists. A new route to the KW-6002 family of antagonists is presented inc...
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PMID: 20652178
PDF is available here.
PDF is available here.
Abstract
A range of amide derivatives of L-dopa were synthesized and investigated for their pharmacological activity and their ability to be converted to L-dopa using the unilaterally 6-hydroxydopamine (6-OHDA)-lesioned rat, as an experimental model of Parkinson's disease. The diacetyl derivative of L-dopa a...
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PMID: 20646792
PDF is available here.
PDF is available here.
Clinical Oncology (22)7 2010
Abstract
We present our results of CRT for LAPC using capecitabine and delivering radiotherapy to a limited radiation field that excluded non-involved regional lymph nodes from the clinical target volume.
Thirty patients were studied. Patients received 50.4 Gy external beam radiotherapy in 28 fractions, deli...
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PMID: 20650619
PDF is available here.
PDF is available here.
Chemical Communications (46)31 2010
Abstract
In contrast to amidines bearing ionizable alpha-CH bonds, which react with nitric oxide (NO) to add diazeniumdiolate groups at their alpha-carbons, benzamidine forms an N-bound diazeniumdiolate that can be further derivatized at the other amidine nitrogen and/or the terminal oxygen to form caged NO...
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PMID: 20589293
PDF is available here.
PDF is available here.
Abstract
We designed and prepared a series of hydroxamate analogues bearing a tertiary amine. Enzyme assays using JMJD2C, JMJD2A, and prolyl hydroxylases revealed that hydroxamate analogue 8 is a potent and selective JMJD2 inhibitor, showing 500-fold greater JMJD2C-inhibitory activity and more than 9100-fold...
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PMID: 20684604
PDF is available here.
PDF is available here.
Abstract
We present an overview of the GST inhibitors and the GST-activated pro-drugs utilized to date to overcome drug resistance.
2010 Elsevier Inc. All rights reserved....
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PMID: 20494652
PDF is available here.
PDF is available here.
Abstract
We report an adenosine nucleoside prodrug that potently inhibits DENV replication both in cell culture and in a DENV mouse model. NITD449 (2'-C-acetylene-7-deaza-7-carbamoyladenosine) was initially identified as a parental compound that inhibits all four serotypes of DENV with low cytotoxicity. Howe...
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PMID: 20516277
PDF is available here.
PDF is available here.
Abstract
The hepatitis C virus (HCV) NS5B RNA polymerase facilitates the RNA synthesis step during the HCV replication cycle. Nucleoside analogs targeting the NS5B provide an attractive approach to treating HCV infections because of their high barrier to resistance and pan-genotype activity. PSI-7851, a pron...
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PMID: 20516278
PDF is available here.
PDF is available here.
Abstract
A series of oxazolidine-based compounds with a variety of substituents in positions 2 and 3 was synthesized and their stability studied. Ring opened intermediates formed on addition of limiting amounts of D(2)O to oxazolidine solutions, as observed by NMR. As the hydrolysis reactions...
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PMID: 20229599
PDF is available here.
PDF is available here.
Inflammopharmacology (18)4 2010
Abstract
The present study was designed to evaluate, P2026 [(2-((2-(nitrooxy)ethyl)disulfanyl)ethyl 2-(2-(2,6-dichlorophenylamino)phenyl)acetate)], a novel NO (nitric oxide) donor prodrug of diclofenac for its ability to release NO and diclofenac, and whether P2026 provides advantage of improved activity/gas...
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PMID: 20495878
PDF is available here.
PDF is available here.
Arthritis & Rheumatism (62)7 2010
Abstract
We found that inhibition of Syk in MRL/lpr and BAK/BAX mice prevented the development of skin disease and significantly reduced established skin disease. Similarly, Syk inhibition reduced the size of the spleen and lymph nodes, suppressed the development of renal disease, and suppressed established...
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PMID: 20222110
PDF is available here.
PDF is available here.
FASEB Journal (24)7 2010
Abstract
Synthetic nanoparticle formulations have the potential for tumor-targeted gene delivery. Receptor-targeted nanocomplex (RTN) formulations comprise mixtures of cationic liposomes and targeting peptides that self-assemble on mixing with nucleic acids. RTN formulations were prepared containing differen...
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PMID: 20203088
PDF is available here.
PDF is available here.
Arbaclofen placarbil decreases postprandial reflux in patients with gastroesophageal reflux disease.
Abstract
AP decreased reflux and associated symptoms with good tolerability in patients with GERD....
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PMID: 20040914
PDF is available here.
PDF is available here.
Abstract
To enhance the stability of the anticancer drug gemcitabine (2'-deoxy-2',2'-difluorocytidine), it was conjugated to poly-l-glutamic acid (PG-H) via a carbodiimide reaction. The synthesised poly-l-glutamic acid-gemcitabine (PG-G) was purified and characterised by using SDS-PAGE to estimate its molecu...
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PMID: 20214970
PDF is available here.
PDF is available here.
Abstract
A novel mutual prodrug consisting of 4-biphenylacetic acid (BPA) and quercetin tetramethyl ether (QTME) has been synthesized as a gastrosparing NSAID, devoid of ulcerogenic side effects. The physicochemical properties, including aqueous solubility, partition coefficient, chemical stability and enzym...
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PMID: 20227799
PDF is available here.
PDF is available here.
CNS Spectrums (15)5 2010
Abstract
Attention-deficit/hyperactivity disorder (ADHD) is a highly genetic neuropsychiatric disorder that can cause impairment at school, work, home, and in social relationships. Once considered a childhood disorder, as many as 65% of children with ADHD continue to exhibit symptoms into adulthood. While a...
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PMID: 20448522
PDF is available here.
PDF is available here.
Abstract
N(3)-o-toluyl-fluorouracil weakly inhibited the proliferation of SMMC-7721 and PLC/PRF/5 cells in the absence of liver microsomal enzymes. In contrast, the inhibition rates were significantly increased in the presence of these enzymes. HPLC results revealed that TFU was metabolized slowly by liver m...
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PMID: 19756602
PDF is available here.
PDF is available here.
Abstract
Abstract
For the purpose of reducing the strong CYP3A4 inhibitory potency of diamide prodrug 4, cyclic prodrugs of tricyclic-based FBPase inhibitors were synthesized. Extensive SAR studies led to the discovery of pyridine-containing cyclic prodrug 20, which strongly inhibited glucose production in monkey hep...
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PMID: 20359891
PDF is available here.
PDF is available here.
Abstract
We propose a new prodrug strategy for improved delivery of nucleoside analogues to ameliorate their biological efficacy.
2010 Elsevier Ltd. All rights reserved....
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PMID: 20363623
PDF is available here.
PDF is available here.
Abstract
The design and study of two classes of noncompetitive acetylcholinesterase inhibitors (AChEIs) which also function as NSAID prodrugs are reported. The most potent AChEIs disclosed contain an aromatic alkyl-aryl linker between an NSAID and a lipophilic choline mimic and they inhibit acetylcholinester...
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PMID: 20347302
PDF is available here.
PDF is available here.
Journal of Physical Chemistry B (114)14 2010
Abstract
Colistin is an amphiphilic antibiotic that has re-emerged into clinical use due to the increasing prevalence of difficult-to-treat Gram-negative infections. The existence of self-assembling colloids in solutions of colistin and its derivative prodrug, colistin methanesulfonate (CMS), was investigate...
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PMID: 20302384
PDF is available here.
PDF is available here.
Abstract
The synthesis of the first spacer containing, duocarmycin analogue prodrug was realised, its biological properties evaluated and compared to its counterpart prodrug without a spacer unit. The synthesis comprises the manufacture of the new acetylated derivatives and of two double spacer systems, thei...
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PMID: 20449487
PDF is available here.
PDF is available here.
Abstract
The aim of this study was to investigate the lipophilic prodrug as a means of promoting acyclovir (ACV) that exhibited biphasic insolubility into the ethosomes for optimum skin delivery. Acyclovir Palmitate (ACV-C(16)) was synthesized as the lipophilic prodrug of ACV. The ethosomal system and the li...
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PMID: 20422366
PDF is available here.
PDF is available here.
Antiviral Research (86)1 2010
Abstract
We review here the structural and enzymatic properties of the enzymes that carry out the activation of analogs used in therapy against human immunodeficiency virus and against DNA viruses such as hepatitis B, herpes and poxviruses. Four major classes of drugs are considered: thymidine analogs, non-n...
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PMID: 20417378
PDF is available here.
PDF is available here.
Abstract
The first glucuronide prodrug of the hedgehog signaling inhibitor cyclopamine was synthesized. The carbamoyl derivatisation of cyclopamine significantly decreased its toxicity towards the U87 human glioblastoma cell line. However, when the prodrug was incubated with beta-glucuronidase in the culture...
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PMID: 20116904
PDF is available here.
PDF is available here.
Abstract
Capecitabine, an oral prodrug of 5-fluorouracil, is indicated for adjuvant treatment in patients with Dukes' C colon cancer and for subsequent lines in metastatic colorectal cancer. The aim of this article is to review the literature on the economics of capecitabine for the treatment of colon cancer...
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PMID: 20384557
PDF is available here.
PDF is available here.
Bioanalysis (2)4 2010
Abstract
Bioanalytical support of drug-discovery efforts increasingly requires more complex multiple component analysis, including the bioanalysis of drugs, prodrugs and metabolites. Just as the physiochemical properties of these components may differ widely from each other, optimal LC and MS...
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PMID: 21083272
PDF is available here.
PDF is available here.
Abstract
Modifying FTY720, an immunosuppressant modulator, led to a new series of well phosphorylated tetralin analogs as potent S1P1 receptor agonists. The stereochemistry effect of tetralin ring was probed, and (-)-(R)-2-amino-2-((S)-6-octyl-1,2,3,4-tetrahydronaphthalen-2-yl)propan-1-ol was identified as a...
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PMID: 20188554
PDF is available here.
PDF is available here.
Abstract
We demonstrate a new concept directly using drug molecules to fabricate nanocarriers in order to minimize use of inert materials, substantially increase the drug loading content, and suppress premature burst release. Taking advantage of the strong hydrophobicity of the anticancer drug camptothecin (...
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PMID: 20218672
PDF is available here.
PDF is available here.
Abstract
5-Fluorouracil-1-acetic acid (5-FUA) was prepared and covalently conjugated to beta-cyclodextrin (beta-CyD) through ester or amide linkage, and the drug release behavior of the conjugates in enzymatic solutions and rat cecal contents were investigated. The 5-FUA/beta-CyD ester conjugate was slowly h...
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PMID: 20036722
PDF is available here.
PDF is available here.
Abstract
Intra-observer and inter-observer tumor volume measurements show no significant differences. No differences were found between T1 and T2 volume tumor doubling times between the three sham groups. A significant statistical difference (p<0.05) in T1 and T2 volume tumor doubling times between the three...
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PMID: 20338540
PDF is available here.
PDF is available here.
Clinical Therapeutics (32)3 2010
Abstract
The generic and branded formulations of MMF 500 mg met the European regulatory criteria for assuming bioequivalence, based on the rate and extent of absorption of a single dose under fasting conditions. Both formulations were well tolerated in these healthy volunteers.
Copyright 2010 Excerpta Medic...
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PMID: 20399993
PDF is available here.
PDF is available here.
Pharmacotherapy (30)3 2010
Abstract
We summarize the genetic causes of clopidogrel nonresponsiveness, with a focus on larger outcomes-based studies. A MEDLINE search of the English-language literature (1990-2008) was conducted to identify studies that examined these relationships; additional citations were obtained from the articles r...
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PMID: 20180610
PDF is available here.
PDF is available here.
Pharmacotherapy (30)3 2010
Abstract
We reviewed recently published reports of trials that examined the interaction. A MEDLINE database search (1966-September 2009) for English-language reports of clinical trials in human subjects was performed, supplemented by a manual search of reference lists. Four trials that examined surrogate out...
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PMID: 20180611
PDF is available here.
PDF is available here.
Xenobiotica (40)3 2010
Abstract
These results demonstrated that CS-8958 administered intratracheally to rats was converted/hydrolysed to R-125489 in the target tissues, and that the R-125489 was slowly excreted into the urine via an absorption rate-limiting process. Such distinctive pharmacokinetics attributed to the slow release...
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PMID: 20146556
PDF is available here.
PDF is available here.
Bulletin du cancer (97)3 2010
Abstract
Tamoxifen is a prodrug mainly metabolized by the CY2D6 cytochrome. More than 80 variants of the CYP2D6 gene have been identified. They predict four different enzymatic phenotypes: ultra-rapid metabolizers (UM), extensive metabolizers (EM), intermediate metabolizers (IM) and poor metabolizers (PM). S...
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PMID: 20123649
PDF is available here.
PDF is available here.
Abstract
Thirty-seven patients were eligible for safety and efficacy. TMN staging at baseline was: T4N2, 11%; T3N2, 40%; T2N2, 3%; T3N1, 35%; T2N1, 3% and T3N0 8%. The most common adverse events included, grade 1/2 acneiform skin rash (86%), and grade 3 radiodermatitis, (16%), diarrhea (11%) and hypersensiti...
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PMID: 20042310
PDF is available here.
PDF is available here.
Abstract
Our results suggest that the antinociceptive effect of indomethacin or acemetacin is not mediated by NO or K+ channel activation.
2010 Prous Science, S.A.U. or its licensors. All rights reserved....
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PMID: 20401346
PDF is available here.
PDF is available here.
Abstract
Reduced glutathione (GSH) is the most abundant non-protein thiol in mammalian cells and the preferred substrate for several enzymes in xenobiotic metabolism and antioxidant defense. It plays an important role in many cellular processes, such as cell differentiation, proliferation and apoptosis. GSH...
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PMID: 20335977
PDF is available here.
PDF is available here.
Chemical Communications (46)8 2010
Abstract
Matrix metalloproteinase inhibitors (MMPi) possessing a glucose protecting group on the zinc-binding group (ZBG) show a dramatic increase in inhibitory activity upon cleavage by beta-glucosidase.
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PMID: 20449263
PDF is available here.
PDF is available here.
Pharmacogenomics (11)3 2010
Abstract
Recent developments in a number of molecular profiling technologies, including genomic/genetic testing, proteomic profiling and metabolomic analysis have allowed the development of 'personalized medicine'. Irinotecan is one of the models for personalized medicine based on pharmacogenetics, and a num...
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PMID: 20235794
PDF is available here.
PDF is available here.
Future Oncology (6)3 2010
Abstract
The hypoxic cells common in solid tumors (because of their inefficient blood supply) limit the effectiveness of radiotherapy and many cytotoxic drugs. Nontoxic prodrugs that generate active species in hypoxic tissue by selective bioreduction have long been explored, and the first examples, represent...
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PMID: 20222798
PDF is available here.
PDF is available here.
Abstract
We designed a multi-protected L-DOPA prodrugs able to release the drug by both spontaneous chemical or enzyme catalyzed hydrolysis. The new compounds have been synthesized and preliminarily evaluated for their water solubility, log P, chemical stability, and enzymatic stability. The results indicate...
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PMID: 20153654
PDF is available here.
PDF is available here.
Abstract
Esterification of xylan with ibuprofen via activiation of the carboxylic acid with N,N'-carbonyldiimidazole (CDI) yields products of high drug loadings. Subsequent sulfation of xylan ibuprofen esters using the gentle agent SO(3)/DMF was successfully carried out in order to modify hyd...
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PMID: 19904721
PDF is available here.
PDF is available here.
Abstract
Esterification of xylan with ibuprofen via activiation of the carboxylic acid with N,N'-carbonyldiimidazole (CDI) yields products of high drug loadings. Subsequent sulfation of xylan ibuprofen esters using the gentle agent SO(3)/DMF was successfully carried out in order to modify hyd...
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PMID: 19904721
PDF is available here.
PDF is available here.
Abstract
Esterification of xylan with ibuprofen via activiation of the carboxylic acid with N,N'-carbonyldiimidazole (CDI) yields products of high drug loadings. Subsequent sulfation of xylan ibuprofen esters using the gentle agent SO(3)/DMF was successfully carried out in order to modify hyd...
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PMID: 19904721
PDF is available here.
PDF is available here.
Oncology Reports (23)2 2010
Abstract
We developed a new, sensitive isocratic-elution HPLC method for quantifying ara-GTP. Samples were eluted isocratically by using phosphate buffer at a constant flow rate. Ara-GTP was clearly separated from other nucleotides by using an anion-exchange column and it was quantitated by its peak area at...
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PMID: 20043113
PDF is available here.
PDF is available here.
Abstract
We proposed a novel method for predicting the absorption of prodrugs in the absence of CES-mediated hydrolysis in Caco-2 cells. The specific inhibition against CES was achieved using bis-p-nitrophenyl phosphate (BNPP). The optimal concentration of BNPP was determined at 200 microM by measuring the t...
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PMID: 19923255
PDF is available here.
PDF is available here.