title: 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.
authors.affiliation: Research and Development, Farmitalia-Carlo Erba, Erbamont Group, Milan, Italy.
authors.forename: F M
authors.initials: FM
authors.lastname: Arcamone
authors.forename: F
authors.initials: F
authors.lastname: Animati
authors.forename: B
authors.initials: B
authors.lastname: Barbieri
authors.forename: E
authors.initials: E
authors.lastname: Configliacchi
authors.forename: R
authors.initials: R
authors.lastname: D'Alessio
authors.forename: C
authors.initials: C
authors.lastname: Geroni
authors.forename: F C
authors.initials: FC
authors.lastname: Giuliani
authors.forename: E
authors.initials: E
authors.lastname: Lazzari
authors.forename: M
authors.initials: M
authors.lastname: Menozzi
authors.forename: N
authors.initials: N
authors.lastname: Mongelli
mesh_terms: D000477:Alkylating Agents; D000818:Animals; D055598:Chemical Phenomena; D002621:Chemistry; D002851:Chromatography, High Pressure Liquid; D002942:Circular Dichroism; D004247:DNA / Q000378:metabolism*; D004214:Distamycins / Q000138:chemical synthesis / Q000378:metabolism / Q000627:therapeutic use; D006801:Humans; D007939:Leukemia L1210 / Q000188:drug therapy; D007942:Leukemia, Experimental / Q000188:drug therapy; D051379:Mice; D009369:Neoplasms / Q000188:drug therapy*; D011758:Pyrroles / Q000138:chemical synthesis / Q000378:metabolism / Q000627:therapeutic use; D013329:Structure-Activity Relationship; D014407:Tumor Cells, Cultured
chemical_list: D000477:Alkylating Agents; D004214:Distamycins; D011758:Pyrroles; D004247:DNA