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At least 73 records · Page 4Linked to original sources
PubMed1979

Chemosensitivity of human bladder cancer cells in long-term culture and clinical responses to the selected anticancer drug.

In vitro sensitivity of an established cell line from human urinary bladder cancer to various chemotherapeutic agents was determined by 14C-leucine incorporation into the target cells. Of 12 drugs tested, Carboquone, Neocarzinostatin, Actinomycin D, Adriamycin, Mitomycin C and Chromomycin A3 produced intensive cytotoxic effects, while Thio-Tepa, Bleomycin, 5-Fluorouracil and Vincirstine were less cytotoxic, Intravesical instillation of Carboquone, one of the most toxic agents in vitro, resulted in complete or partial tumor remission in 6 of 9 patients with bladder cancer. Prophylactic effects of periodic intravesical Carboquone were also indicated in 7 of 8 patients who had experienced recurring superficial bladder tumors.

Antineoplastic Agents↗
PubMed1985

Aziridinylbenzoquinone in recurrent, progressive glioma of the central nervous system. A Phase II study by the Illinois Cancer Council.

Aziridinylbenzoquinone (AZQ) was studied in a Phase II protocol for persons with glioma of the central nervous system (CNS) recurrent or progressive after surgery and radiotherapy. Patients received AZQ, 30 mg/m2 intravenously every 3 weeks if previously untreated or 27.5 mg/m2 if previously exposed to cytotoxic drugs. Partial response was defined as a reduction of at least 50% reduction in the product of the two longest perpendicular diameters of the indicator lesion persisting for a minimum of 28 days. Twenty-eight patients are evaluable for response at this time. Objective response (OR) occurred in four (14.3%): two complete and two partial. Stabilization of disease (SD) was seen in 7 (25.0%). Median survival, in weeks, was greater than 46.0 for responders, 41.7 for SD, and 19.3 for those with progressive disease. The survival experiences are significantly different (P = 0.030 [Breslow]). The OR rate was 21.1% in 19 without prior chemotherapy and 0% in 9 previously treated patients. There were two AZQ-related deaths in patients with prior exposure to nitrosoureas (1 CNS hemorrhage; 1 aspiration pneumonia). One patient had an anaphylactic reaction. Three patients whose tumor initially increased in size subsequently had marked tumor shrinkage. AZQ is an active agent that must be used with added caution in patients who have received nitrosoureas. Initial tumor enlargement may precede response. Although response appears to prolong survival, the correlation between stabilization of disease and survival is not well-defined.

Adolescent↗
PubMed1983

Specific labelling of the hydrophobic domain of rat renal gamma-glutamyltransferase.

The amphipathic form of gamma-glutamyltransferase (EC 2.3.2.2) was reconstituted into unilamellar lecithin vesicles and labelled using the membrane-soluble reagent, 3-trifluoromethyl-3-(m-[125I]iodophenyl)diazirine ( [125I]TID), which can be photoactivated. Label was incorporated exclusively into the large subunit of the transferase, but no label was found in the enzyme released from the vesicles by partial proteolysis with papain. Chromatography of the papain-treated vesicles on Sephadex LH-60 indicated that the [125I]TID was bound to two peptides of low relative molecular mass. The [125I]-TID-labelled peptides should constitute the hydrophobic membrane-binding domain. The transferase was also labelled by reductive methylation (Lys residues) or with immobilized galactose oxidase and NaB3H4 (Gal residues), incorporated into lecithin vesicles and treated with papain. Both procedures yielded a single [3H]-labelled hydrophobic peptide that remained associated with the vesicles. After chromatography on Sephadex LH-60, the peptide labelled by the latter two procedures corresponds to the larger of the two [125I]TID-labelled peptides. These results suggest that papain may cleave the hydrophobic domain into two peptides. The observed labelling is also consistent with the alternative possibility that the N-terminal hydrophobic domain is preceded by an initial sequence that contains both lysine and carbohydrate residues. The smaller of the two [125I]TID-labelled peptides could be generated by removal of the hydrophilic segment from the transferase molecules that are reconstituted with the N-terminus exposed on the external surface of the vesicles.

Amino Acid Sequence↗
PubMed1980

Mass spectrometry as a technique for testing the purity of drugs for biological use: the case of new antitumor cyclophosphazenes.

Mass spectrometry has been used for testing the chemical purity of some new antitumor cyclophosphazene compounds. the spectrum of N3P3Az6 (code name MYKO 63)--which exhibits noticeable activity on murine P 388, L 1210 and B 16 tumors--appeared to be remarkably simple, as most of the fragmentations arose from successive losses of the aziridino radicals. Traces of the pentaziridinomonochloro impurity formed by an incomplete substitution of N3P3Cl6 chlorine atoms under aziridinolysis could be detected in an impure and toxic sample by spectral subtraction. Quantification of this impurity was performed by selected ion monitoring in the direct inlet mode of sample introduction. The mass spectra of other derivatives of this class of compounds are slightly more complex, since the decomposition pathways showed more intense H-transfers associated with the loss of substituents.

Antineoplastic Agents↗