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

Abstract
A group of potential alkylating agents 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.
AuthorsF M Arcamone, F Animati, B Barbieri, E Configliacchi, R D'Alessio, C Geroni, F C Giuliani, E Lazzari, M Menozzi, N Mongelli
JournalJournal of medicinal chemistry (J Med Chem) Vol. 32 Issue 4 Pg. 774-8 (Apr 1989) ISSN: 0022-2623 [Print] United States
PMID2590277 (Publication Type: Comparative Study, Journal Article)
Chemical References
  • Alkylating Agents
  • Distamycins
  • Pyrroles
  • DNA
Topics
  • Alkylating Agents
  • Animals
  • Chemical Phenomena
  • Chemistry
  • Chromatography, High Pressure Liquid
  • Circular Dichroism
  • DNA (metabolism)
  • Distamycins (chemical synthesis, metabolism, therapeutic use)
  • Humans
  • Leukemia L1210 (drug therapy)
  • Leukemia, Experimental (drug therapy)
  • Mice
  • Neoplasms (drug therapy)
  • Pyrroles (chemical synthesis, metabolism, therapeutic use)
  • Structure-Activity Relationship
  • Tumor Cells, Cultured

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