Sulfonamides known as inhibitors of many metabolic enzymes have been widely used as antimicrobial drugs for a long time. In the present study, we investigated in vitro inhibitory activities of benzenesulfonamide derivatives on human paraoxonase-I (hPON1). For this aim, PON1 was purified from human serum with a specific activity of 2603.57 EU/mg and 8.34% yield using simple chromatographic methods. The various concentrations of early-synthesized sixteen sulfonamide derivatives were tested on the paraoxonase activity. K-i values of compounds were found in the range of 0.28-357.70 mu M. Compound H4 had the highest inhibitory activity on hPON1 as competitive. Estimated structure-activity relationship (SAR) for compounds was done based on different substituents and their positions in the compounds. Besides, the molecular docking analysis of compound H4 was performed to understand the binding interactions on the active site of the enzyme. According to these experimental results, compound H4 was a ...

2-amino-N-(quinolin-8-yl)benzenesulfonamide; CAS Number: 16082-64-7; Linear Formula: C15H13N3O2S; find Liverpool ChiroChem-LIVH93E9FC02 MSDS, related peer-reviewed papers, technical documents, similar products & more at Sigma-Aldrich

A novel series of benzenesulfonamide derivatives containing 4-aminobenzenesul-fonamide and α-amides branched valproic acid or 2,2-dimethylcyclopropanecarboxylic acid moieties were synthesized and screened for their anticonvulsant activities in mice maximal electroshock seizure (MES) and subcutaneous pentylenetetrazole (scPTZ) test. The activity experimental study showed that 2,2-dipropyl-N1-(4-sulfamoylphenyl)malonamide (18b) had the lowest median effective dose (ED50) of 16.36 mg/kg in MES test, and 2,2-dimethyl-N-(4-sulfamoylphenyl)cyclopropane-1,1-dicarboxamide (12c) had the lowest ED50 of 22.50 mg/kg in scPTZ test, which resulted in the protective indexe (PI) of 24.8 and 20.4, respectively. These promising data suggest the new compounds have good potential as new class of anticonvulsant agents with high effectiveness and low toxicity for the treatment of epilepsy.

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Benzenesulfonamide 98-10-2 NMR spectrum, Benzenesulfonamide H-NMR spectral analysis, Benzenesulfonamide C-NMR spectral analysis ect.

Sulfonamides are the first effective chemotherapeutic agents used for several years to cure or prevent systemic bacterial infections. In addition, this agents showed anti-carbonic anhydrase and cause cell cycle perturbation in the G1 phase, disruption of microtubule assembly, suppression of the transcription activator Nf-Y, angiogenesis and matrix metalloproteinase (MMP). In recent years, novel synthesized sulfonamides have been introduced as antitumor, antiviral and anti-inflammatory agents. In this paper, the cytotoxic effects of 8 synthesized sulfonamides were investigated by MTT assay on HeLa, MDA-MD-468 and MCF-7 cancer cell lines. Human cancer cells were cultured and passaged in RPMI-1640 medium. Cells incubated in 96-well plates in a concentration of 1 × 105 cells/mL for 24 h, and then logarithmic concentrations (0.1 µm, 1 µm, 10 µm, 100 µm, 1mM) of each drug were prepared, added to the plates and incubated for 72 h. Cell survival was then determined using ELISA plate reader in 540 nm

Sulfonamides will be the initial effective chemotherapeutic brokers used for quite some time to remedy or prevent systemic bacterial attacks. in 540 nm applying MTT assay. All examined sulfonamides demonstrated cytotoxic influence on HeLa and MCF-7 cells in the focus selection of 100-1000 m. These sulfonamides had been cytotoxic against MDA-MB-468 cell collection at a focus of 10-100 m and decreased the cell success significantly less than 50%. Based on the outcomes calculated IC50s had been as pursuing: MDA-MB-468 30 m; MCF-7 128 m and HeLa RAB7A 360 m. To conclude, some examined sulfonamides had great cytotoxic results against breast malignancy cells, MDA-MB-468 and additional investigations are had a need to confirm their results against various other cells. strong course=kwd-title KEY TERM: Sulfonamides, MTT assay, MDA-MB-468, HeLa, MCF-7 Launch Sulfonamide was the first antimicrobial medication that its chemical substance moiety can be present in various other medications that are not ...

JNST (ISSN: 2455-0191) - JACS Directory- Abstract: The title compound methyl (2E)-2-{[N-(2-formylphenyl)-4-methylbenzene sulfonamido] methyl}-3- phenylprop-2-enoate (MFMSPE) is a derivative of sulfonamide. FT-IR spectra of MFMSPE in the solid phase were recorded and analyzed. The optimized geometry and vibrational wave numbers were computed using DFT/B3LYP method with aid of 6-311++G (d,p) basis set. Stability of the molecule arising from hyper conjugative interactions, charge delocalization has been analyzed using natural bond orbital (NBO) analysis. The calculated HOMO and LUMO energies confirm that charge transfer occurs within the molecule. Molecular electrostatic potentials (MEP) was carried out at and interpreted. To recognize the biological activity of MFMSPE, molecular docking was done to recognize the hydrogen bond lengths and binding energy with antibacterial protein (1KE4). Keywords: DFT Calculation; NBO; Molecular Docking; - Journal of Nanoscience and Technology.

Quinoline derivatives have diverse biological activities including anticancer activity. On the other hand, many sulfonamide derivatives exhibited good cytotoxic activity. Hybrids of both moieties may present novel anticancer agents. Chloroquinoline incorporating a biologically active benzene-sulfonamide moieties 5-21 and diarylsulfone derivatives 22 and 23 were prepared using (E)-1-(4-((E)-7-chloro-1-methylquinolin-4(1H)-ylideneamino)phenyl)-3-(dimethyl-amino)prop-2-en-1-one 4 as strategic starting material. The structure of the newly synthesized compounds were confirmed by elemental analyses and spectral data. Compound 4 was confirmed by X-ray crystallographic analysis. The prepared compounds were evaluated for their anticancer activity against Lung, HeLa, Colorectal and breast cancer cell lines. Compounds 2, 4, 7, 11, 14 and 17 showed better or comparable activity to 2′, 7′-dichlorofluorescein (DCF) as reference drug. Molecular docking of the active compounds on the active site of PI3K enzyme was

We used a targeted PCR of integrons from polluted environmental samples followed by amplicon sequencing using next generation sequencing technologies to greatly extend our knowledge of mobile antibiotic resistance genes found as gene cassettes. Combining the accuracy of short reads from Illumina sequencing with the higher resolution of long reads from PacBio sequencing generated a clear view of the gene cassettes and their immediate context, also providing clues about their evolutionary history. We therefore suggest that a similar approach could be applied to search for ARGs as well as other functional genes in different contexts.. Putative novel ARGs for aminoglycosides, beta-lactams, trimethoprim, rifampicin, chloramphenicol, and sulfonamides were identified. Several novel OXA variants provided reduced susceptibility to carbapenems, providing an additional battery of integron-borne genes that could contribute to resistance against last-line antibiotics. Many of the known and putative ARGs that ...

N-(1H-Imidazole-5-ylmethyl)-N-[4-[4-(benzylcarbamoyl)piperazino]phenyl]benzenesulfonamide | C28H30N6O3S | CID 44282638 - structure, chemical names, physical and chemical properties, classification, patents, literature, biological activities, safety/hazards/toxicity information, supplier lists, and more.

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TYTU : Synthesis, QSAR studies, and metabolic stability of novel 2-alkylthio-4-chloro-N-(5-oxo-4,5-dihydro-1,2,4-triazin-3-yl)benzenesulfonamide derivatives as potential anticancer and apoptosis-inducing agents ...

PRIMARY OBJECTIVES:. I. To assess the feasibility and safety of individualizing pazopanib (pazopanib hydrochloride) monotherapy based upon attained pazopanib plasma concentrations so as to achieve desired target pazopanib plasma concentration in the highest possible fraction of treated patients.. SECONDARY OBJECTIVES:. I. To assess whether patient cytochrome P450 (CYP) or other polymorphisms may correlate with attained pazopanib levels in response to standard pazopanib dosing.. II. To assess whether patient trough pazopanib levels attained 24 hours after initiation of 800 mg daily fasting may predict steady state trough pazopanib levels after 14 days of pazopanib administration.. III. To assess whether patient trough pazopanib levels may correlate with observed pazopanib toxicities.. OUTLINE: This is a dose-escalation study.. Patients receive pazopanib hydrochloride orally (PO) once daily (QD) on days 1-28. Courses repeat every 28 days in the absence of disease progression or unacceptable ...

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This study presents the synthesis of nineteen 1-(substitutedbenzoyl)-4- benzhydrylpiperazine and 1-[(substitutedphenyl)sulfonyl]-4-benzhydrylpiperazine derivatives. In vitro cytotoxic activities of the compounds were screened against hepatocellular (HUH-7), breast (MCF-7) and colorectal (HCT-116) cancer cell lines by sulphorhodamine B assay. Among the test compounds, benzamide derivatives had high cytotoxic activity whereas sulfonamide derivatives showed variable 50% growth inhibition (GI50). © Georg Thieme Verlag KG Stuttgart · New York ...

The high-resolution solution structure of the catalytic fragment of humancollagenase-3 (MMP-13) complexed with a sulfonamide derivative of ahydroxamic acid compound (WAY-151693) has been determined bymultidimensional heteronuclear NMR. A total of 30 structures werecalculated for residues 7-164 by means of hybrid distancegeometry-simulated annealing using a total of 3280 experimental NMRrestraints. The atomic rms distribution about the mean coordinatepositions for the 30 structures is 0.43(+/-0.05) A for the backbone atoms,0.80(+/-0.09) A for all atoms, and 0.47(+/-0.04) A for all atoms excludingdisordered side-chains. The overall structure of MMP-13 is composed of abeta-sheet consisting of five beta-strands in a mixed parallel andanti-parallel arrangement and three alpha-helices where its overall foldis consistent with previously solved MMP structures. A comparison of theNMR structure of MMP-13 with the published 1.6 A resolution X-raystructure indicates that the major differences between the ...

The invention relates to sulfonamide derivatives, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. More parti

A profound analysis of the industry based on the N-tert-butyl-benzothiazole Sulfonamide (TBBS) Market all over the world is named as Global N-tert-butyl-benzothiazole Sulfonamide (TBBS) Market Report. The research report assesses the current as well as the upcoming performance of the N-tert-butyl-benzothiazole Sulfonamide (TBBS) market, in addition to with newest trends in the market. The major player of the N-tert-butyl-benzothiazole Sulfonamide (TBBS) market (Lanxess, Eastman, Agrofert, KUMHO PETROCHEMICAL, Arkema, Kemai Chemical, Sunsine, Shandong Yanggu Huatai Chemical, Jiangsu Sinorgchem Technology, Puyang Willing Chemicals, Sumitomo Chemical, Sanshin, King Industries, Stairchem)are also included in the market report. The report forecasts the future of the N-tert-butyl-benzothiazole Sulfonamide (TBBS) market on the basis of this evaluation.. The research analysis for N-tert-butyl-benzothiazole Sulfonamide (TBBS) market comprises each and every feature of the market all over the world, ...

[Vitamins and metabolism of sulfonamides. I. Behavior of the sulfonamide levels in the body fluids and tissues of guinea pigs after loading with B complex vitam

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ACID-CATALYZED REACTION OF PHENOLS WITH N -(4,4-DIETHOXYBUTYL)SULFONAMIDES - A NEW METHOD FOR THE SYNTHESIS OF 2-ARYL-1-SULFONYLPYRROLIDINES

ment, separation, and detection of the analytes were identifiedand optimized. The pH of the sample proved to be the mostinfluential variable during sample extraction. A critical impact onthe retention of the analytes on the cartridge material wasobserved, especially for sulfonamides caused by their aminogroups. Our enrichment tests between pH 2 and 6 revealed, asexpected, highest recoveries at pH 4 for the sulfonamides, whilethe recovery of the macrolides and trimethoprim showed nostrong pH dependence. This behavior can be explained by thecharge state of the sulfonamides at the particular pH values (Table1).26-31 With a compound specific pKa of 5-8 for the sulfonaminogroups (pKa 1) and a pKa of 2-2.5 for the arylamin (pKa 2), thesulfonamides are positively charged at pH 2 and negatively at a shows the breakdown curves for N4AcSMX and its four most pH above 5. The interaction with the cartridge material is strongest intense fragments as a function of the collision energy. As for analytes in ...

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Sulfonamide antibiotics have been used to combat a wide spectrum of bacterial infections ever since the discovery of Prontosil in 1932.

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De cerebrale doorbloeding is globaal verlaagd in patiënten met Multiple Sclerose (MS) en kan op zijn beurt bijdragen tot de progressieve axonale degeneratie, cognitieve achteruitgang en vermoeidheid. In deze placebo-gecontrolleerde dubbel-blinde gerandomiseerde studie met de endotheline-1 antagonist bosentan, willen we graag nagaan of het pharmacologische herstel van de cerebrale blood flow (CBF) in patiënten met MS het axonaal metabolism en de klinische achteruitgang kan verbeteren ...

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Compounds 9 and 11 were also noted as attractive, novel compounds in their own right. These were used for very limited library construction. The compounds derived from 9 were profiled first. While better than the parent bromide, subsequent structural analysis showed that they were not making good interactions with the sites intended (WPF shelf). The sulfonamides derived from 11 on the other hand showed significantly improved activity. The SAR was relatively insensitive to the substitution of the aryl group, due to the optimized placement on the shelf and the reversed sulfonamide ...

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Sickle cell disease is a highly prevalent disease in the United States, affecting 1 in 500 African American infants. It is common in individuals of African, Caribbean, Mediterranean, Arab, and other Middle Eastern descent. It is a genetic disorder with an autosomal recessive inheritance pattern. Sickle cell disease is often called the first molecular disease because the biochemical alteration in sickle hemoglobin described by Linus Pauling in 1948 was one of the first lesions identified at the molecular level for a human disease. Sickle hemoglobin forms rod-like polymers in deoxygenated red cells in areas of the circulation, with low oxygen tension, acidosis, or hyperosmolarity. Sickle hemoglobin polymerization causes a host of secondary molecular and cellular changes, many of which impair blood flow and contribute to tissue damage. The microcirculation can be acutely or chronically impaired in virtually any organ in the body, resulting in the characteristic crisis pattern of intermittent pain ...

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Title:Dosimetry and Toxicity Studies of the Novel Sulfonamide Derivative of Sulforhodamine 101([18F]SRF101) at a Preclinical Level. VOLUME: 12 ISSUE: 1. Author(s):Ingrid Kreimerman, Erick Mora-Ramirez, Laura Reyes, Manuel Bardiès, Eduardo Savio* and Henry Engler. Affiliation:Uruguayan Centre of Molecular Imaging (CUDIM), Radiopharmacy Department, Montevideo, Inserm, UMR1037 CRCT, F-31000 Toulouse, Uruguayan Centre of Molecular Imaging (CUDIM), Radiopharmacy Department, Montevideo, Inserm, UMR1037 CRCT, F-31000 Toulouse, Uruguayan Centre of Molecular Imaging (CUDIM), Radiopharmacy Department, Montevideo, Uruguayan Centre of Molecular Imaging (CUDIM), Radiopharmacy Department, Montevideo. Keywords:Preclinical evaluation, toxicity, dosimetry, [18F]SRF101, PET radiotracers, tissue-weighting factors.. Abstract:Background: The SR101 N-(3-[18F]Fluoropropyl) sulfonamide ([18F]SRF101) is a Sulforhodamine 101 derivative that was previously synthesised by our group. The fluorescent dye SR101 has been ...

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The purpose of the study is to investigate the possible benefits of giving the anti-HIV drug maraviroc to people who are taking darunavir/ritonavir alone for their HIV treatment. Many people successfully take only darunavir/ritonavir treatment for their HIV. However, there are some concerns that this treatment may not reach some areas of the body, such as the brain and spinal cord (central nervous system or CNS), as effectively as it does the bloodstream.. There is already a large clinical study looking at any differences between conventional HIV treatment with 3 drugs and single drug treatment with a protease inhibitor, also called PI monotherapy, such as darunavir/ritonavir. This includes differences in the effects on the CNS. However, this study will only be finished in 2013.. The investigators know that maraviroc can reach the CNS very effectively. The investigators in this study will investigate the effect of adding maraviroc to darunavir/ritonavir monotherapy by looking at levels of ...

TY - JOUR. T1 - 2-Amino-N-{4-[5-(2-phenanthrenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl] -phenyl} acetamide (OSU-03012), a celecoxib derivative, directly targets p21-activated kinase. AU - Porchia, Leonardo M.. AU - Guerra, Marcy. AU - Wang, Yu Chieh. AU - Zhang, Yunlong. AU - Espinosa, Allan V.. AU - Shinohara, Motoo. AU - Kulp, Samuel K.. AU - Kirschner, Lawrence S.. AU - Saji, Motoyasu. AU - Chen, Ching Shih. AU - Ringel, Matthew D.. PY - 2007/11. Y1 - 2007/11. N2 - p21-Activated kinases (PAKs) are regulators of cell motility and proliferation. PAK activity is regulated in part by phosphoinositide-dependent kinase 1 (PDK1). We hypothesized that reduced PAK activity was involved in the effects of 2-amino-N-{4-[5-(2-phenanthrenyl)-3-(trifluoromethyl)-1H-pyrazol-1- yl]-phenyl} acetamide (OSU-03012), a previously characterized PDK1 inhibitor derived from celecoxib. In three human thyroid cancer cell lines, OSU-03012 inhibited cell proliferation with reduced AKT phosphorylation by PDK1. OSU-03012 ...

In a previous study, we reported that the short-term treatment with celecoxib, a non-steroidal anti-inflammatory drug (NSAID) attenuates the activation of brain structures related to nociception and does not interfere with orthodontic incisor separation in rats. The conclusion was that celecoxib could possibly be prescribed for pain in orthodontic patients. However, we did not analyze the effects of this drug in periodontium. The aim of this follow-up study was to analyze effects of celecoxib treatment on recruitment and activation of osteoclasts and alveolar bone resorption after inserting an activated orthodontic appliance between the incisors in our rat model. Twenty rats (400-420 g) were pretreated through oral gavage with celecoxib (50 mg/kg) or vehicle (carboxymethylcellulose 0.4%). After 30 min, they received an activated (30 g) orthodontic appliance, set not to cause any palate disjunction. In sham animals, the appliance was immediately removed after introduction. All animals received ...

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Rats administered doses up to 43 mg/kg/day in males and 52 mg/kg/day in females had no increases in tumor incidence, with the exception of a modest increase in the frequency of mammary gland fibroadenomas in female rats receiving doses ≥5.4 mg/kg (P,0.015). The highest doses of tamsulosin hydrochloride evaluated in the rat carcinogenicity study produced systemic exposures (AUC) in rats 3 times the exposures in men receiving the maximum therapeutic dose of 0.8 mg/day.. Mice were administered doses up to 127 mg/kg/day in males and 158 mg/kg/day in females. There were no significant tumor findings in male mice. Female mice treated for 2 years with the two highest doses of 45 and 158 mg/kg/day had statistically significant increases in the incidence of mammary gland fibroadenomas (P,0.0001) and adenocarcinomas (P,0.0075). The highest dose levels of tamsulosin hydrochloride evaluated in the mice carcinogenicity study produced systemic exposures (AUC) in mice 8 times the exposures in men receiving ...

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PubMedID: 24737576 | Acute renal failure associated with the new BRAF inhibitor vemurafenib: A case series of 8 patients. | Cancer | 7/15/2014

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Structure, properties, spectra, suppliers and links for: 4-Methyl-N-[4-(trimethylsilyl)-3-butyn-1-yl]-N-[(trimethylsilyl)ethynyl]benzenesulfonamide.

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It is important to note that sulfone-containing products are non-antibiotic sulfonamides and therefore also lack the N1 heterocyclic ring. Recent investigations into the COX-2 inhibitor, celecoxib, which also lacks the aromatic amine and N1-substituent, did not show any cross-reaction in patients with a sulfonamide antibiotic allergy.11,12 Another example of a sulfone-containing agent is the newer COX-2 inhibitor, etoricoxib (Figure 4),13,14 which is a sulfone and also lacks the aromatic amine and N1-substituent.. It seems most authors agree that non-antibiotics are less likely to cause severe reactions, and that the chemical differences between sulfa-antibiotics and non-antibiotics make true cross-reactivity extremely unlikely. An extensive literature survey found only one case report of anaphylaxis caused by furosemide;15 the authors were not able to prove that the allergen was in fact conclusively chemically related to the sulfa moiety.. Perhaps the most reassuring evidence comes from Strom ...

Several studies suggest that cyclooxygenase (COX)-2 plays a pivotal role in the progression of ischemic brain damage. In the present study, we investigated the effects of selective inhibition of COX-2 with nimesulide (12 mg/kg) and selective inhibition of COX-1 with valeryl salicylate (VAS, 12-120 mg/kg) on prostaglandin E2 (PGE2) levels, myeloperoxidase (MPO) activity, Evans Blue (EB) extravasation and infarct volume in a standardized model of transient focal cerebral ischemia in the rat. Postischemic treatment with nimesulide markedly reduced the increase in PGE2 levels in the ischemic cerebral cortex 24 h after stroke and diminished infarct size by 48 % with respect to vehicle-treated animals after 3 days of reperfusion. Furthermore, nimesulide significantly attenuated the blood-brain barrier (BBB) damage and leukocyte infiltration (as measured by EB leakage and MPO activity, respectively) seen at 48 h after the initial ischemic episode. These studies provide the first experimental evidence ...

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No. Therefore sulfonamides are selectively toxic to bacteria and other microorganisms. Against which microorganisms are sulfonamides effective? Gram-positive and gram-negative bacteria, Nocardia, Chlamydia trachomatis, some protozoa (malaria), Escherichia Coli, Klebsiella, Salmonella, Shigella, Enterobacter Are sulfonamide antibiotics bactericidal or bacteriostatic? Primarily bacteriostatic What are the adverse effects of sulfonamide antibiotics? Nausea; vomiting; diarrhea; phototoxicity; hemolysis (in individuals having glucose-6-phosphate dehydrogenase (G6PD) deficiency); hypersensitivity; Stevens-Johnson syndrome (incidence and severity of adverse effects greatly increase immunocompromised in AIDS patients) Why are sulfonamide antibiotics contraindicated in neonates? 25% How much drug is left after three half-lives? 5% During constant infusion, what percent of steady state is reached after one half-life? 50% During constant infusion, what percent of steady state is reached after two ...

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The sulfonamides are weakly acidic compounds that have a common chemical nucleus resembling p-aminobenzoic acid (PABA). Members of this group differ mainly in their pharmacokinetic properties and clinical uses. Pharmacokinetic features include modest tissue penetration, hepatic metabolism, and excretion of both intact drug and acetylated metabolites in the urine. Solubility may be decreased in acidic urine, resulting in precipitation of the drug or its metabolites. Because of the solubility limitation, a combination of 3 separate sulfonamides ...

These studies indicate that laromustine readily undergoes base-catalyzed (nonenzymatic) conversion to methylisocyanate and 90CE, which further degrade to additional chloroethylating derivatives. Figure 1B shows the proposed formation of decomposition/metabolite product pathways of laromustine formed in in vitro systems. The rate at which [14C]laromustine (100 μ M) produces its metabolites/degradation products in the presence of NADPH-fortified HLMs was essentially the same as that in the absence of NADPH or the presence of boiled (heat-denatured) microsomes. Additionally, it remained consistent with the nonenzymatic rate of laromustine degradation in potassium phosphate buffer (Nassar et al., 2009). This suggests that laromustine metabolism/degradation is not significantly affected by human liver microsomal P450 enzymes and carboxylesterases.. Only the formation of C-7 required the presence of NADPH. C-7 appears to be decomposed or metabolized further, which suggests that P450 is a factor in ...

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