Thymine, 1 - , antitumor activity

The first, in vivo study on the antitumor activity of ketonucleosides appeared14 in 1977. The action of l-(6-deoxy-2,3-0-isopropylidene-a-L-h/xo-hexopyranosyl-4-ulose)thymine (45) and of 7-(3-0-acetyl-4,6-dideoxy-/ -L-gfi/cero-hex-3-enopyranosyl-2-ulose)theophylline (61a) against LI 210 leukemia in mice was examined comparatively. From the results obtained, it was clear that the unsaturated ketohexosylpurine 61a was much more active than the ketohexosylpyrimidine 45, whereas the parent nucleosides (44 and 34a, respectively) were inactive under the same experimental conditions. 

Ruiz J, Lorenzo J, Sanglas L, Cutillas N, Vicente C, Villa MD, Aviles FX, Lopez G, Moreno V, Perez J, Bautista D (2006) Palladium(II) and platinum(II) organometallic complexes with the model nucleobase anions of thymine, uracil, and cytosine antitumor activity and interactions with DNA of the platinum compounds. Inorg Chem 45 6347-6360... 

In this connection it is important to note that the unusual arabinosyl derivatives of thymine and uracil (222 and 223), so far detected in only one sponge species, Cryptotethya crypta 18), have served as a model for the synthesis of D-arabinosylcytosine, which has potent anticancer activity it inhibits the growth of Sarcoma 180, Ehrlich carcinoma and L-1210 Leukemia in mice 63, 64, 124). However, human tests of this compound for antitumor activity have been disappointing 175). 

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