3-deazauridine and Brain-Neoplasms

3-deazauridine has been researched along with Brain-Neoplasms* in 2 studies

Other Studies

2 other study(ies) available for 3-deazauridine and Brain-Neoplasms

Article	Year
High-pressure liquid chromatographic analysis of 3-deazauridine-5'-triphosphate in human cancer cells. Cancer treatment reports, 1979, Volume: 63, Issue:3 A rapid high-pressure liquid chromatographic assay for the detection and quantitation of 3-deazauridine-5'-triphosphate (deazaUTP), the active metabolite of the anticancer drug 3-deazauridine (deazaUrd), in cell extracts is described. This procedure permits the simultaneous detection and quantitation of CTP, the cellular concentration of which is affected by treatment with deazaUrd. Human lymphoblastoid cells (line CCRF-CEM) treated with 100 nmols of deazaUrd/ml in culture accumulate deazaUTP to greater than 25 nmols/10(7) cells after 4 hours. The concentration of CTP in these cells decreased exponentially with a half-life of 1.1 hours. After these cells had been incubated with 100 nmols of deazaUrd/ml and were resuspended in drug-free medium, the intracellular deazaUTP concentration decreased exponentially with a half-life of 3.4 hours. This assay has been applied to clinical studies of deazaUrd; high cellular deazaUTP concentrations have been detected in brain tumor tissue after deazaUrd infusion. Topics: 3-Deazauridine; Brain Neoplasms; Chromatography, High Pressure Liquid; Humans; In Vitro Techniques; Leukemia, Lymphoid; Male; Middle Aged; Neoplasms; Neoplasms, Experimental; Nucleotides; Time Factors; Uridine; Uridine Triphosphate	1979
Penetration of 3-deazauridine into human brain, intracerebral tumor, and cerebrospinal fluid. Cancer research, 1979, Volume: 39, Issue:10 The antitumor agent 3-deazauridine (DAU) was administered rapidly to four patients before surgical removal of intracerebral tumor. Tumor, adjacent brain tissue, and temporalis muscle were assayed for DAU by high-pressure liquid chromatography. DAU penetrated comparably into tumor, brain, and muscle; in one patient, tissue concentrations were higher than concurrent plasma concentrations. The active metabolite 3-deazauridine 5'-triphosphate was quantitated in one tumor sample and greatly exceeded its Ki for cytidine 5'-triphosphate synthetase. DAU was also present in autopsy brain specimens from two patients treated shortly antemortem. Cerebrospinal fluid concentrations were 22.1 and 59.0%, respectively, of concurrent plasma concentrations during continuous infusion of DAU in two patients. Cerebrospinal fluid concentration was 3.1 microgram/ml 2 hr after a 30-min infusion of 1.5 g of drug per sq m and fell to 1.9 microgram/ml at 16 hr. Thus, DAU is capable of penetrating into intracerebral tumor, brain, and cerebrospinal fluid and is worthy of investigation in the treatment of intracerebral and meningeal neoplasms. Topics: 3-Deazauridine; Blood-Brain Barrier; Brain; Brain Neoplasms; Humans; Meningeal Neoplasms; Muscles; Uridine	1979

Article

Year

High-pressure liquid chromatographic analysis of 3-deazauridine-5'-triphosphate in human cancer cells.

Cancer treatment reports, 1979, Volume: 63, Issue:3

A rapid high-pressure liquid chromatographic assay for the detection and quantitation of 3-deazauridine-5'-triphosphate (deazaUTP), the active metabolite of the anticancer drug 3-deazauridine (deazaUrd), in cell extracts is described. This procedure permits the simultaneous detection and quantitation of CTP, the cellular concentration of which is affected by treatment with deazaUrd. Human lymphoblastoid cells (line CCRF-CEM) treated with 100 nmols of deazaUrd/ml in culture accumulate deazaUTP to greater than 25 nmols/10(7) cells after 4 hours. The concentration of CTP in these cells decreased exponentially with a half-life of 1.1 hours. After these cells had been incubated with 100 nmols of deazaUrd/ml and were resuspended in drug-free medium, the intracellular deazaUTP concentration decreased exponentially with a half-life of 3.4 hours. This assay has been applied to clinical studies of deazaUrd; high cellular deazaUTP concentrations have been detected in brain tumor tissue after deazaUrd infusion.

Topics: 3-Deazauridine; Brain Neoplasms; Chromatography, High Pressure Liquid; Humans; In Vitro Techniques; Leukemia, Lymphoid; Male; Middle Aged; Neoplasms; Neoplasms, Experimental; Nucleotides; Time Factors; Uridine; Uridine Triphosphate

1979

Penetration of 3-deazauridine into human brain, intracerebral tumor, and cerebrospinal fluid.

Cancer research, 1979, Volume: 39, Issue:10

The antitumor agent 3-deazauridine (DAU) was administered rapidly to four patients before surgical removal of intracerebral tumor. Tumor, adjacent brain tissue, and temporalis muscle were assayed for DAU by high-pressure liquid chromatography. DAU penetrated comparably into tumor, brain, and muscle; in one patient, tissue concentrations were higher than concurrent plasma concentrations. The active metabolite 3-deazauridine 5'-triphosphate was quantitated in one tumor sample and greatly exceeded its Ki for cytidine 5'-triphosphate synthetase. DAU was also present in autopsy brain specimens from two patients treated shortly antemortem. Cerebrospinal fluid concentrations were 22.1 and 59.0%, respectively, of concurrent plasma concentrations during continuous infusion of DAU in two patients. Cerebrospinal fluid concentration was 3.1 microgram/ml 2 hr after a 30-min infusion of 1.5 g of drug per sq m and fell to 1.9 microgram/ml at 16 hr. Thus, DAU is capable of penetrating into intracerebral tumor, brain, and cerebrospinal fluid and is worthy of investigation in the treatment of intracerebral and meningeal neoplasms.

Topics: 3-Deazauridine; Blood-Brain Barrier; Brain; Brain Neoplasms; Humans; Meningeal Neoplasms; Muscles; Uridine

1979