Bioorganic & medicinal chemistry letters

Esters of 2-(1-hydroxyalkyl)-1, 4-dihydroxy-9, 10-anthraquinones with melphalan as multifunctional anticancer agents

GZ Jin, YJ You, BZ Ahn

Index: Jin, Guang-Zhu; You, Young-Jae; Ahn, Byung-Zun Bioorganic and Medicinal Chemistry Letters, 2001 , vol. 11, # 11 p. 1473 - 1476

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Citation Number: 9

Abstract

Eight esters of 2-(1-hydroxyalkyl)-1, 4-dihydroxy-9, 10-anthraquinone with melphalan were prepared and tested for their antitumor activity (S-180) and cytotoxicity. 2-{1-[4-(p-Bis (2- chloroethyl)-aminophenyl)-butanoyloxy] methyl}-1, 4-dihydroxy-9, 10-anthraquinone and 2- {1-[4-(p-bis (2-chloroethyl)-aminophenyl)-butanoyloxy] ethyl}-1, 4-dihydroxy-9, 10- anthraquinone showed remarkable antitumor activity (T/C, 265 and 272%).