| 摘要 |
<p>Daunorubicin deriv. of formula (I) and its acid-addn. salts are new: (where X is OPO)OH)2). (I) is prepd. by reacting 14-bromo-daunorubicin, i.e. (I) where X = Br, with a quat. ammonium phosphate of formula Me(R)3N+OPO(OR')2 (where R' is H or a protecting gp., pref. T-Bu, and each R is independently 1-4C alkyl), opt. followed by deprotection and/or salt formation. (I) has antitumour activity and low toxicity, e.g. with an effective dose of 0.25mg/kg. (i.p.) against leukaemia L1210 in mice and a maximum tolerance dose of 2mg/kg.</p> |
