Abstract |
In vitro antitumor activities of 13 saframycins, including the potent antitumor component, saframycin A, were determined with the highly sensitive established cell line of L1210 mouse leukemia to investigate structure-activity relationships. Saframycins which lack the alpha-cyanoamine group or the alpha-carbinolamine group exhibited much lower cytotoxic activity than saframycin A. The modification of active saframycins either at the C-14 position on the basic skeleton or at the C-25 position on the side chain with bulky substituents resulted in a decrease in cytotoxic activity. These structure-activity relationships corroborated the proposed major mechanism of action for the antitumor activity of saframycin A and supported our proposed model for the saframycin A- DNA adduct.
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Authors | K Kishi, K Yazawa, K Takahashi, Y Mikami, T Arai |
Journal | The Journal of antibiotics
(J Antibiot (Tokyo))
Vol. 37
Issue 8
Pg. 847-52
(Aug 1984)
ISSN: 0021-8820 [Print] England |
PMID | 6480503
(Publication Type: Journal Article)
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Chemical References |
- Antibiotics, Antineoplastic
- Isoquinolines
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Topics |
- Animals
- Antibiotics, Antineoplastic
- Cell Line
- Isoquinolines
(pharmacology)
- Leukemia L1210
(drug therapy)
- Magnetic Resonance Spectroscopy
- Mice
- Models, Molecular
- Structure-Activity Relationship
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