Influence of (22R)-22-aminocholesterol on cholesterol metabolism in rats.
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Biomedical subjects
Publications and source records attributed to Y Letourneux.
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Various new aminosterols were synthesized. The antiproliferative activity of these compounds (I-IV) was studied in vitro on a continuous human non small-cell bronchopulmonary carcinoma line (NSCLC-N6) at the cell cycle level. The histograms indicate cell blockage in Phase Gl (compound I-III) associated with a reduction in the number of cells phases S and G2M and appearance of cellular debris derived from cells in Phase G1.
L1210 leukemia was used to evaluate the antitumour activity in vivo of CY233 (NSC 609224) a new water-soluble nitrosoureido derivative of deoxysugar currently being studied in preclinical trials. The antitumour activity of CY233 is dose-dependent with the same large therapeutic index whatever the route of administration (I.P., I.V., per os). Thus starting from a single dose of 10 mg/kg (less than 25% of the LD50), 80% to 100% of mice survive at 120 days, whether the drug is being administered I.V., I.P. or P.O. These results clearly emphasize the very original and promising potentiality of CY233 among the series of alkylating agents, and more precisely nitrosoureas.