Synthesis, DNA-binding properties, and antitumor activity of novel distamycin derivatives

…, B Barbieri, E Configliacchi, R D'Alessio…

文献索引：Arcamone, Federico Maria; Animati, Fabio; Barbieri, Brunella; Configliacchi, Emanuela; D'Alessio, Roberto; et al. Journal of Medicinal Chemistry, 1989 , vol. 32, # 4 p. 774 - 778

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被引用次数: 158

摘要

A group of potential alkylating agenta have been synthesized that are structurally related to the oligopeptide antiviral antibiotic distamycin. All derivatives form complexes with native calf-thymus DNA but compounds 2, 3, and 6 give rise to covalent adducts. Cytostatic activity against both human and murine tumor cell lines in vitro is displayed by the new compounds. Compounds 3 and 4 are active on melphalan-resistant L1210 leukemia in mice.