Antitumor effects of bis-thiosemicarbazones— inhibition of deoxyribonucleic acid synthesis in vitro |
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Authors: | David Kessel R Stanley McElhinney |
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Institution: | 1. Michigan Cancer Foundation, Wayne State University School of Medicine, USA;2. Medical Research Council of Ireland, Trinity College, Dublin, Ireland |
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Abstract: | A group of bis-thiosemicarbazones was evaluated for potential antitumor activity, using the L1210 murine leukemia in cell culture. Drug levels required to inhibit DNA synthesis by 50 per cent, under standard conditions, were determined. The most potent of the agents examined had the structure XCH2CR1=NNHCSNHR2]2 where X = C or S and R1 = R2 = CH3. Optimal activity was also obtained with R1 = H and R2 = CH3 only when X = S. The most potent derivatives inhibited DNA synthesis by 50 per cent within 10 min at 10?6 M levels (id50). Metal chelates of several compounds tested were extremely potent inhibitors of DNA synthesis (). Insolubility in water and short duration of action in vivo may limit effectiveness of the bis-thiosemicarbazones. |
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Keywords: | Requests for reprints: Darling Memorial Center 4160 John R Street Detroit Mich (48201) |
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