“…The synergistic effects might be due to the exploitation of the above-mentioned individual properties of T/C% = Mean median survival of the drug-treated animals (T) versus corn-oil-treated controls (C). 4 D/2!3 = LD 10 /2 given i.p. at the 1st, 5th and 9th day after tumor transplantation.…”
Section: Discussionmentioning
confidence: 99%
“…The solvent was removed under reduced pressure and the residue was chromatographed on silica gel. Elution with chloroform gave the desired compound with an 81% yield vs. 62% [4], m.p. (ethylacetate) 119-120°C vs. 118-121°C [4].…”
Section: Synthesis Proceduresmentioning
confidence: 99%
“…Elution with chloroform gave the desired compound with an 81% yield vs. 62% [4], m.p. (ethylacetate) 119-120°C vs. 118-121°C [4]. All spectral analyses (IR, NMR and mass spectrometry were identical.…”
Section: Synthesis Proceduresmentioning
confidence: 99%
“…The compound ASE was prepared by a new method which gave a better yield and sorter reaction time than the method described in the literature [4]. This new method was as follows: 1.5 g (5.4 mmol) of 4-N,Nbis(2-chloroethyl)aminophenylacetic acid were dissolved in 30 ml of dry benzene.…”
The authors studied the effect of two modified steroids containing different proportions (%) of alkylating agents alone or in combination on sister chromatid exchange (SCE) rates and on human lymphocyte proliferation kinetics. The antitumor activity of these compounds was tested on leukemia P388- and leukemia L1210-bearing mice. The two chemicals in mixtures enhance SCE induction and antitumor activity in a synergistic manner. The homo-aza-steroidal ester of p-bis(2-chloroethyl)aminophenyl acetic acid was found to be more effective than the homo-aza-steroidal ester of o-bis(2-chloroethyl)aminobenzoic acid in causing cytogenetic damage and antineoplastic activity. A correlation was observed between the magnitude of the SCE response and the depression of the cell proliferation index. The order of the antitumor effectiveness of the five different treatments tested coincided with the order of the cytogenetic effects they induced.
“…The synergistic effects might be due to the exploitation of the above-mentioned individual properties of T/C% = Mean median survival of the drug-treated animals (T) versus corn-oil-treated controls (C). 4 D/2!3 = LD 10 /2 given i.p. at the 1st, 5th and 9th day after tumor transplantation.…”
Section: Discussionmentioning
confidence: 99%
“…The solvent was removed under reduced pressure and the residue was chromatographed on silica gel. Elution with chloroform gave the desired compound with an 81% yield vs. 62% [4], m.p. (ethylacetate) 119-120°C vs. 118-121°C [4].…”
Section: Synthesis Proceduresmentioning
confidence: 99%
“…Elution with chloroform gave the desired compound with an 81% yield vs. 62% [4], m.p. (ethylacetate) 119-120°C vs. 118-121°C [4]. All spectral analyses (IR, NMR and mass spectrometry were identical.…”
Section: Synthesis Proceduresmentioning
confidence: 99%
“…The compound ASE was prepared by a new method which gave a better yield and sorter reaction time than the method described in the literature [4]. This new method was as follows: 1.5 g (5.4 mmol) of 4-N,Nbis(2-chloroethyl)aminophenylacetic acid were dissolved in 30 ml of dry benzene.…”
The authors studied the effect of two modified steroids containing different proportions (%) of alkylating agents alone or in combination on sister chromatid exchange (SCE) rates and on human lymphocyte proliferation kinetics. The antitumor activity of these compounds was tested on leukemia P388- and leukemia L1210-bearing mice. The two chemicals in mixtures enhance SCE induction and antitumor activity in a synergistic manner. The homo-aza-steroidal ester of p-bis(2-chloroethyl)aminophenyl acetic acid was found to be more effective than the homo-aza-steroidal ester of o-bis(2-chloroethyl)aminobenzoic acid in causing cytogenetic damage and antineoplastic activity. A correlation was observed between the magnitude of the SCE response and the depression of the cell proliferation index. The order of the antitumor effectiveness of the five different treatments tested coincided with the order of the cytogenetic effects they induced.
“…Our research has involved the synthesis of steroidal lactams [1] or lactones [2] esterified with carboxylic derivatives of N,N-bis(2-chloroethyl)aniline and study of these compounds, for antitumor activity [3,5], This report further defines the antineoplastic activ ity of 3/?-hydroxy-13a-amino-13,17-seco-5a-androstan-17-oic-13,17-lactam-/>-bis(2-chloroethyl)aminophenoxyacetate (NSC 294859) in animal tumors.…”
3β-hydroxy-13α-amino-13,17-seco-5α-androstan-17-oic-13,17-lactam-p-bis(2-chloroethyl)amino-phenoxyacetate, a modified steroidal alkylating agent, is active in the treatment of colon 26 tumor, B16 melanoma and P388 leukemia.
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