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BHAC is a newly synthesized lipophilic derivative of ara-C. To clarify its pharmacological mode of action, P388 murine leukemic cells were incubated with two different types of 14C-labeled BHAC, [cytosine-2-14C]BHAC and [acyl-1-14C]BHAC, and DNA was extracted with phenol. The phenol-extracted DNA was then hydrolyzed by nuclease P1 and analyzed with high-performance liquid chromatography (HPLC). The radioactivity of DNA, from the cells incubated with [cytosine-2-14C]BHAC, was detected as ara-CMP. But the radioactivity of DNA, from the cells incubated with [acyl-1-14C]BHAC, was hardly detected. On the other hand, the main radioactivity of the acid soluble fraction was determined as ara-CTP. On the basis of our results, BHAC is not phosphorylated directly to produce N4-behenoyl-ara-CTP, but is mainly converted to ara-C which subsequently produces ara-CTP, the active metabolite of the drug, and which is then incorporated into DNA.
M Higashigawa, and
H Ochiai, and
T Ohkubo, and
H Kawasaki, and
T Nobori, and
H Kamiya, and
M Sakurai
August 1977,
Cancer research,
M Higashigawa, and
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T Ohkubo, and
H Kawasaki, and
T Nobori, and
H Kamiya, and
M Sakurai
January 1981,
Recent results in cancer research. Fortschritte der Krebsforschung. Progres dans les recherches sur le cancer,
M Higashigawa, and
H Ochiai, and
T Ohkubo, and
H Kawasaki, and
T Nobori, and
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M Sakurai
January 1980,
Recent results in cancer research. Fortschritte der Krebsforschung. Progres dans les recherches sur le cancer,
M Higashigawa, and
H Ochiai, and
T Ohkubo, and
H Kawasaki, and
T Nobori, and
H Kamiya, and
M Sakurai
October 1988,
Gan to kagaku ryoho. Cancer & chemotherapy,
M Higashigawa, and
H Ochiai, and
T Ohkubo, and
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M Sakurai
January 1989,
Chemotherapy,
M Higashigawa, and
H Ochiai, and
T Ohkubo, and
H Kawasaki, and
T Nobori, and
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M Sakurai
January 1989,
Anticancer research,
M Higashigawa, and
H Ochiai, and
T Ohkubo, and
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September 1987,
[Rinsho ketsueki] The Japanese journal of clinical hematology,
M Higashigawa, and
H Ochiai, and
T Ohkubo, and
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H Kamiya, and
M Sakurai
June 1983,
Gan,
M Higashigawa, and
H Ochiai, and
T Ohkubo, and
H Kawasaki, and
T Nobori, and
H Kamiya, and
M Sakurai
June 1981,
Cancer research,
M Higashigawa, and
H Ochiai, and
T Ohkubo, and
H Kawasaki, and
T Nobori, and
H Kamiya, and
M Sakurai
June 1987,
Gan to kagaku ryoho. Cancer & chemotherapy,
