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Esters of chlorambucil with 2-substituted 1,4-dihydroxy-9,10-anthraquinones as multifunctional anticancer agents

Authors
Journal
European Journal of Medicinal Chemistry
0223-5234
Publisher
Elsevier
Publication Date
Volume
36
Issue
4
Identifiers
DOI: 10.1016/s0223-5234(01)01229-6
Keywords
  • Anthraquinone
  • Chlorambucil
  • Ester
  • Cytotoxicity
  • Antitumor
  • Structure–Activity Relationship

Abstract

Abstract Novel twelve esters of chlorambucil with 2-(1-hydroxyalkyl)-1,4-dihydroxy-9,10-anthraquinone were synthesized and tested for their antitumor activity in mice bearing S-180 ascitic cells as well as cytotoxic activity against L1210 cells. Eight of them were highly cytotoxic on L1210 cells (ED 50, <6 μg mL −1) and derivatives 1 and 12 (T/C, 200 and 205%) appeared more active in vivo than chlorambucil (T/C, 168%).

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