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At least 1,009 records · Page 56Linked to original sources
PubMed1977

Cellular response to treatment with 4-(3-(2-chloroethyl)-3-nitrosoureido)-cis-cyclohexanecarboxylic acid, a water-soluble nitrosourea derivative.

The lethal effects of 4-(3-(2-chloroethyl)-3-nitrosoureido)-cis-cyclohexanecarboxylic acid (cis-acid), a water-soluble nitrosourea derivative, were investigated on a human lymphoma cell line. The survival of asynchronous cells exposed to increasing concentrations of the drug was characterized by a threshold exponential curve (Do = 20 microgram/ml; Dq = 20 microgram/ml, 1 hour) similar to that of other nitrosourea derivatives. cis-Acid exerted its main killing effect on cells in early S and in late G2 phase. Cells in mid S and early G1 phase were tenfold more resistant. Changes in survival response as a function of cell cycle stage were reflected primarily by changes in the extent of the shoulder region of the survival curve. In contrast to other nitrosoureas, the lethal effectiveness of cis-acid in solution was stable and the drug could sterilize large numbers of cells in short periods of time. Another important major difference observed for cis-acid with respect to classic nitrosourea derivatives was the capacity of treated cells to recover from sublethal and potentially lethal damage. Our studies have shown that cis-acid is as effective in killing cultured human lymphoma cells as other nitrosoureas, but possibly with a mechanism different from that of these compounds. The major shortcoming noted for cis-acid, namely the capacity of treated cells to recover from drug-induced damage, is offset by the relatively long stability of its killing effect. This, and the fact that cis-acid can be administered in an aqueous solution, make this agent an appealing compound for clinical trials.

Antineoplastic Agents↗
PubMed1989

[Antibacterial action of some saturated and unsaturated long-chain carboxylic acids and their bis(2-chloroethyl)aminoethyl esters in vitro].

Using the method of twofold serial dilution of substances in liquid nutrient medium with subsequent reseeding on solid nutrient medium a comparative study has been carried out of the antibacterial action in vitro of long chain saturated (C10-C18) and unsaturated (C11-C22) carboxylic acids and their bis(2-chloroethyl)aminoethyl esters against Pseudomonas aeruginosa, Klebsiella pneumoniae tp 16 Koph, Escherichia coli ATCC 25922, Staphylococcus aureus 101+ and Proteus mirabilis 56. The compounds studied have an inhibitory effect upon the development of the microorganisms. The minimum inhibitory concentration ranges from 1.8 to 19.3 mumol/ml. There exists a linear correlation between the length of the carbon chain (the number of C atoms) of the compounds and the minimum inhibitory concentration in the following cases: esters of saturated acids (C16-C24) and unsaturated acids (C11-C22) against Pseudomonas aeruginosa; unsaturated acids (C11-C22) against Klebsiella pneumoniae tp 16 Koph; esters of unsaturated acids (C17-C28) against Staphylococcus aureus 101+. This correlation has not been found in all other compounds against Escherichia coli ATCC 25922 and Proteus mirabilis 56.

Anti-Bacterial Agents↗
PubMed1991

Genotoxic effect of the antitumour agent homo-aza-steroidal ester of p-bis-(2-chloroethyl)aminophenoxy acetic acid (NSC 294859) tested in the Drosophila wing somatic mutation and recombination test.

The genotoxic activity of the new antineoplastic alkylating agent 3 beta-hydroxy-13 alpha-amino-13,17-seco-5 alpha-androstan-17-oic-13,17- lactam-p-bis-(2-chloroethyl) aminophenoxyacetate (NSC 294859) was studied in the somatic mutation and recombination test (SMART) in Drosophila melanogaster. The drug was administered to larvae which were transheterozygous for two recessive wing cell markers mwh and flr3. Several concentrations were tested and two of them showed a clear induction of mosaic spots, expressing the mutant phenotypes. Multiple wing hair (mwh) spots were the main type observed but twin spots and flares (flr3) spots were also detected. We conclude that the compound induces both mutations and somatic recombination in the SMART test.

Animals↗
PubMed1976

The absorption metabolism, and excretion of Estracyt (NSC 89199) in patients with prostatic cancer.

Estraumustine phosphate (estradiol, 3-N-[bis(2-chloroethyl)-] carbamate-17beta-dihydrogenphosphate (Estracyt) labeled with 3H in the estradiol moiety and 14C in the carbamate moiety was synthesized, and its absorption, metabolism, and excretion were studied after oral administration to three patients with prostatic carcinoma. One of the patients was also given the same dose by intravenous injection. In addition to monitoring isotope levels in peripheral blood, urine, and feces, samples of portal vein blood were obtained through a catheter in the umbilical vein. Analyses of portal blood samples revealed that most of the estramustine phosphate was dephosphorylated to estramustine during absorption. Estramustine was found to be the major metabolite in peripheral blood after oral as well as after intravenous administration. The urinary excretion data appeared to warrent the conclusion that most of the carbamate ester of estraumustine is hydrolyzed before it is excreted. In the patient given estramustine phosphate by both routes the absorption of the compound when given by mouth was found to be approximately 75 per cent.

Administration, Oral↗
PubMed1979

A new steroidal alkylating agent with improved activity in advanced murine leukemias.

The homo-aza-steroidal ester of [p-[bis(2-chloroethyl)amino]phenoxy] acetic acid, 3 beta-hydroxy 13 alpha - amino - 13,17 - seco - 5 alpha-androstan-17-oic-13,17-lactam-p-bis(2-chloroethyl)aminophenoxyacetate, gave a 100% increase in lifespan over controls in the treatment of L1210 leukemia by IP administration on a days 1 and 4 treatment schedule. This ester gave a maximum activity of 383% increased lifespan over controls in the treatment of P388 leukemia by IP administration on a daily treatment schedule. Activity in advanced L1210 (41% increased lifespan) and P388 leukemias (173% increased lifespan) was maintained, indicating that this compound is the most promising of a number of congeners tested to date.

Alkylating Agents↗
PubMedDate not supplied

[The influence of cyclophosphane and phenthyrine and their combination with zymosan and serotonin on the functional features distingusihing peritoneal macrophages in mice].

Radiometric analysis into phagocytic activity of macrophages in intact and tumourous mice following introduction to them of phenthyrine and cyclophosphane showed the former to suppress to a greater extent the absorption function and the latter--that of digestion. A combined application of phenthyrine and cyclophosphane together with serotonin helps re-establish the microphages function in tumourous animals and to heighten the antineplastic activity of these compounds. Zymosan and its combination with phenthyrine and cyclophosphane do not produce any positive effect on the peritoneal cells.

Animals↗
PubMed1977

Treatment of advanced prostatic carcinoma with estramustine phosphate (Estracyt).

Estramustine phosphate (Estracyt) was used in the treatment of 154 patients with carcinoma of the prostate in stage IV. Sixty-three patients were given Estracyt from the outset (primary treatment group) and 91 had previously received some other endocrine therapy (secondary treatment group). All of the patients were observed for more than one year. The drug was given intravenously and/or orally. Objective remissions occurred in 46 (73.0%) of the 63 patients in the primary treatment group and subjective remissions in all the objective responders and in 12 additional patients (92.0%). The corresponding figures for the secondary treatment group were 28 (30.7%) and 52 (57.1%) of 91. The side-effects were negligible, and the drug was well tolerated. No cumulative toxic effect was observed in patients who had been receiving the treatment for more than five years. In our opinion the compound is valuable in the treatment of advanced prostatic carcinoma (stage IV).

Acid Phosphatase↗
PubMed1976

Studies on 4-hydroperoxycyclophosphamide (NSC-181815): a simple preparation method and its application for the synthesis of a new class of "activated" sulfur-containing cyclophosphamide (NSC-26271) derivatives.

4-Hydroperoxycyclophosphamide was obtained in approximately 20% yield by ozonization of cyclophosphamide in acetone/water at 0 degrees C. It was reduced to 4-hydroxycyclophosphamide, which was treated with several mercaptans to yield compounds of the type 4-(S-R)-mercapto-cyclophosphamide. In the solid state these compounds are stable at room temperature; in aqueous solution they are hydrolyzed to 4-hydroxycyclophosphamide or its tautomer, aldophosphamide. One of the 4-(S-R)-mercapto-cyclophosphamide compounds was tested biologically in vitro against Yoshida ascites tumor cells and showed the same cytotoxic activity as 4-hydroxycyclophosphamide.

Alkylating Agents↗