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»õ·Î¿î Anthracycline°è Ç×¾ÏÁ¦ DA-125ÀÇ È°¼­±âÀü¿¡ °üÇÑ ¿¬±¸(I) Mechanism of Antitumor Activity of DA-125, a New Anthracycline Antibiotics(I)

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Abstract

From various new anthracylines containing fluorine in their sugar moieties, 7-0-(2,6-dideoxy-2-fluoro-a-1-talopyranosyl)-adriamycinone-14-¥â-alaninate•HCl(DA-125) has been selected for clinical investigation, because of its excellent antitumor
acitivity
and low toxicity. In this paper the mechanism whereby DA-125 exhibits good antitumor activity in vivo was studied through in vitro experiments in comparison with doxorubicin(DXR). DA-125 had stronger activity than DXR in single and double strand
scission in P388 cells and in inhibition of nucleic acid synthesis in L1210 cells. But DA-125 had weaker activity than DXR in binding to calf thymus DNA. DA-125 was taken up by P388 cells faster than DXR and accumulated reaching at 2.7 fold
higher
level.

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