PURPOSE: To obtain a new aminoanthraquinone compound useful as an anti- tumor agent having reduced toxicity while retaining strong anti-tumor activity.
CONSTITUTION: A compound of formula I [R1 is H, a lower alkyl or a lower alkoxy; R2 is H; R3 is H, OH, a lower alkyl, a lower alkoxy, thiol, a lower alkylthio, NH2, a primary or secondary lower alkylamino or R3 and R2 are bonded to form (CH2)nA-(A is O or S; n is 1-3); formula II is single bond or double bond; R4 is H or a lower alkyl when formula II is single bond and R4 is O when formula II is double bond; m is 0-3) or its pharmacologically permissible salt such as 1,4-bis[[2-[(2-hydroxyethyl)amino]ethyl]-5-hydroxy-8- methoxymethylanthraquinone-dihydrochloride. The compound is obtained by reacting a compound of formula III (R7 and R8 are H or an amino-protecting group; R9 is H or an OH-protecting group) with a compound of formula IV (X is a halogen) is the presence of an acid scavenger and deprotecting.
MANABE SHUNICHI
AGARI SHINICHI
SUZUKI MASANOBU
YAMAMOTO YOSHIHISA
UCHIDA ITSURO
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