Synthesis, DNA-binding properties, and antitumor activity of novel distamycin derivatives.
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.
Arcamone
F M
FM
Research and Development, Farmitalia-Carlo Erba, Erbamont Group, Milan, Italy.
Animati
F
F
Barbieri
B
B
Configliacchi
E
E
D'Alessio
R
R
Geroni
C
C
Giuliani
F C
FC
Lazzari
E
E
Menozzi
M
M
Mongelli
N
N
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
D000477:Alkylating Agents; D004214:Distamycins; D011758:Pyrroles; D004247:DNA