In the Search for New Anticancer Drugs, V+ Study of the Binding of Spin-Labeled Thio-TEPA to Cells
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چکیده
the incorporation of 3H-thymidine by 5 0 % (IC50) at a dose of 2.6 X 10~4 M in L 1210 and at a dose of 6 X 10~4 M in P 388 murine leukemias. On the basis of cell fractionation studies, compound 2 was found to bind about equally to the cell nuclei, microsomes, and mitochondria. ESR experiments indicate different degrees of immobilization of the label in various fractions. The efficiency of binding of 2 to cells appears to be at least 6 % .
منابع مشابه
In the Search for New Anticancer Drugs, II Antitumor Activity, Toxicity and Electron Spin Resonance of Spin Labeled Thio-TEPA Derivatives
The spin labeled analog of Thio-Tepa, l-oxyl-2,2,6,6-tetramethyl-4-piperidylN,N;N',N'-bis (ethylene )-phosphorodiamidothioate (SL-O-TT), which contains a nitroxyl free radical linked by an oxygen bridge to phosphorus, has antitumor properties against P388 murine leukemia (T/C = 242) and a higher therapeutic ratio (5.15) than its parent compound, Thio-TEPA (2.75). The drug is less toxic to P388 ...
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تاریخ انتشار 2012