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A novel UPLC/MS/MS method for rapid determination of metapristone in rat plasma, a new cancer metastasis chemopreventive agent derived from mifepristone (RU486).
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Mifepristone (RU486) is a chemical abortifacient used by hundreds of millions of women world-wide. It has recently been used in clinical trials for psychotic depression and cancer chemotherapy. Metapristone is the most predominant biological active metabolite of mifepristone, and being developed as
Chemical induction of ovarian tumors in rats.
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The production and pathogenesis of ovarian cancer was investigated in noninbred albino weanling female rats by surgical fixation into the left ovaries of sutures chemically impregnated with the chemical carcinogens formic acid 2-[4-(5-nitro-2-furyl)-2-thiazolyl]hydrazide (FNT), a nitrofuran
Application of UPLC-MS/MS to simultaneously detect four bioactive compounds in the tumour-shrinking decoction (FM1523) for uterine fibroids treatment.
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Development and validation of a UHPLC-MS/MS method for simultaneous quantitation the plasma concentration of Sabarubicin and its alcohol metabolite M3 in Chinese small cell lung cancer patients.
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To support a novel anthracycline agent - Sabarubicin's pharmacokinetics study in Chinese small cell lung cancer patients, a rapid, sensitive, and high throughput ultra-performance liquid chromatography tandem mass spectrometry method using Doxorubicin hydrochloride as internal standard (IS) was
Immunohistochemical identification of canine melanocytic neoplasms with antibodies to melanocytic antigen PNL2 and tyrosinase: comparison with Melan A.
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The immunoreactivity of PNL2 and antityrosinase in formalin-fixed, paraffin-embedded canine melanocytic neoplasms (n = 101) was compared with that of Melan A. Of the 113 samples overall, 106 were positive for PNL2, 101 for Melan A, and 90 for tyrosinase. Six melanomas that were positive for PNL2
Rapid preparation of rare ginsenosides by acid transformation and their structure-activity relationships against cancer cells.
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The anticancer activities of ginsenosides are widely reported. The structure-activity relationship of ginsenosides against cancer is not well elucidated because of the unavailability of these compounds. In this work, we developed a transformation method to rapidly produce rare dehydroxylated
Development and validation of HPLC-MS/MS procedure for determination of 3,4,4',5-tetra-methoxystilbene (DMU-212) and its metabolites in ovarian cancer cells and culture medium.
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The synthetic resveratrol analogue DMU-212 (3,4,4',5-tetramethoxystilbene) has been shown to possess stronger anticancer activity than resveratrol in a variety of tumour cells. To date, there has been no appropriate procedure that would ensure a reliable data about levels of metabolic products of
An optimized LC-MS/MS method for determination of HYNIC-3PRGD2, a new promising imaging agent for tumor targeting, in rat plasma and its application.
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HYNIC-3PRGD2 is used to prepare a new 99mTc-radiolabeled tracer. HYNIC-3PRGD2, which has a high binding affinity for the integrin αvβ3 due to its special structure, has become a promising tumor imaging agent for diagnosis and monitor of the clinical response to therapeutic effects of anti-tumor
LC-ESI-MS/MS evaluation of forced degradation behaviour of silodosin: In vitro anti cancer activity evaluation of silodosin and major degradation products.
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Silodosin (SLD) a novel α1-adrenoceptor antagonist was subjected to forced degradation involving hydrolysis (acidic, alkaline and neutral), oxidative, photolysis and thermal stress, as per ICH specified conditions. The drug underwent significant degradation under hydrolytic (acidic, alkaline and
Quantification of 4'-geranyloxyferulic acid, a new natural colon cancer chemopreventive agent, by HPLC-DAD in grapefruit skin extract.
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Oxyprenylated natural products (isopentenyloxy-, geranyloxy- and the less spread farnesyloxy-compounds and their biosynthetic derivatives) represent a family of secondary metabolites that have been consider for years merely as biosynthetic intermediates of the most abundant C-prenylated derivatives.
LC-MS/MS method for quantitation of the CK2 inhibitor silmitasertib (CX-4945) in human plasma, CSF, and brain tissue, and application to a clinical pharmacokinetic study in children with brain tumors
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Silmitasertib (CX-4945) as a potent and selective inhibitor of CK2 exhibited promising in vitro and in vivo anti-cancer activity. An assay employing cation-exchange solid phase extraction (SPE) followed by LC-MS/MS analysis was successfully developed and validated for the quantitation of
Validation of a sensitive simultaneous LC-MS/MS method for the quantification of novel anti-cancer thiazolidinedione and quinazolin-4-one derivatives in rat plasma and its application in a rat pharmacokinetic study.
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Thiazolidinediones and quinazolin-4-ones compounds, previously known for their activity against Type 2 diabetes and antifungal activity respectively, are currently being investigated for their anti-cancer activity. The determination of pharmacokinetic parameters for these two classes of compounds
A convenient synthesis and molecular modeling study of novel pyrazolo[3,4-d]pyrimidine and pyrazole derivatives as anti-tumor agents.
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An efficient method to obtain ethyl 5-amino-1-tosyl-1H-pyrazole-4-carboxylate (3) was outlined using condensation reactions of 4-methylbenzenesulfonylhydrazide with (E)-ethyl 2-cyano-3-ethoxyacrylate. The cyclocondensation reaction of this substrate and its hydrazide derivative with urea, thiourea,
Decellularized Lymph Node Scaffolding as a Carrier for Dendritic Cells to Induce Anti-Tumor Immunity.
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In recent decades, the decellularized extracellular matrix (ECM) has shown potential as a promising scaffold for tissue regeneration. In this study, an organic acid decellularized lymph node (dLN) was developed as a carrier for dendritic cells (DCs) to induce antitumor immunity. The dLNs were
Histone proteins determined in a human colon cancer by high-performance liquid chromatography and mass spectrometry.
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The application of reversed-phase high-pressure liquid chromatography under gradient conditions and electrospray ion trap mass spectrometry (LC-ESI-MS) to the analysis of global modification levels of core histones is described. The optimised LC-ESI-MS method was applied for the first time to the
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