Dynemicins, new antibiotics with the 1,5-diyn-3-ene and anthraquinone subunit. II. Antitumor activity of dynemicin A and its triacetyl derivative.
Dynemicin A showed extremely potent in vitro cytotoxicity against a variety of murine and human tumor cells. In the experimental animal tumor models implanted ip with P388, L1210 leukemias and B16 melanoma cells, dynemicin A administered ip significantly prolonged life-span of tumor-bearing mice with the wide range of activity. This antibiotic administered iv was also active against iv implanted P388 and L1210 leukemias. In the macromolecule biosynthesis of B16 melanoma cells, dynemicin A inhibited DNA synthesis specifically. The triacetyl derivative exhibited similar in vitro and in vivo antitumor activities to those of the parent antibiotic.
Kamei
H
H
Bristol-Myers Squibb Research Institute, Tokyo, Japan.
Nishiyama
Y
Y
Takahashi
A
A
Obi
Y
Y
Oki
T
T
D000818:Animals; D000880:Anthraquinones / Q000494:pharmacology / Q000633:toxicity; D000903:Antibiotics, Antineoplastic / Q000494:pharmacology* / Q000633:toxicity; D004249:DNA Damage; D053281:Enediynes; D006801:Humans; D007928:Lethal Dose 50; D008297:Male; D051379:Mice; D009374:Neoplasms, Experimental / Q000188:drug therapy; D009696:Nucleic Acids / Q000096:biosynthesis; D014176:Protein Biosynthesis; D014407:Tumor Cells, Cultured / Q000187:drug effects
D000880:Anthraquinones; D000903:Antibiotics, Antineoplastic; D053281:Enediynes; D009696:Nucleic Acids; C061229:dynemicin A