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Carbocyclic inosine as a potent anti-leishmanial agent: the metabolism and selective cytotoxic effects of carbocyclic inosine in promastigotes of Leishmania tropica and Leishmania donovani.
Potentiation of the antitumor activity of 5-trifluoromethyl-2′-deoxyuridine by the use of depot forms of the parent compound
It is observed that the toxicity of CF3dUrd against HeLA cells in culture was 104 times greater for a 24-h treatment as compared with a 1-H treatment at identical concentrations of the drug, which suggests the importance of using a prolonged treatment period, and the divided dosing ofCF3d Urd to L1210-bearing mice was markedly more effective than its single administration.
Action of 5-trifluoromethyl-2'-deoxyuridine on DNA synthesis.
- H. Satake, S. Takeda, A. Matsumura, M. Sasaki, N. Sugimoto, Y. Wataya
- Chemistry, BiologyNucleic acids symposium series
The results suggested that a mechanism of antitumor activity of CF3dUrd is inhibition of DNA replication.
Anti-parasite activity of nucleoside analogues: the metabolism of carbocyclic inosine in promastigotes of Leishmania tropica and Leishmania donovani and its activity against amastigotes of Leishmania…
Carbocyclic inosine was found to be active against L. donovani amastigotes in an in vivo-like cultivation in vitro and provides a mechanism for the parasite-selective toxicity of carbocyClic inOSine.
Inhibition of in vitro DNA chain elongation of 5-trifluoromethyl-2'-deoxyuridine residue in the template.
Results suggested that a mechanism of antitumor activity of CF3dUrd is inhibition of DNA replication.
Antitumor activity of FTC-092, a masked 5-trifluoromethyl-2′-deoxyuridine derivative
FTC-092 appeared to be effective against various transplantable tumors in mice following oral administration, and its activity was superior to that of several other antitumor fluorinated pyrimidines.
Synthesis of a mutagenic nucleoside, 2'-deoxy-2-(p-nitrophenyl)-adenosine.
In order to study structure-activity relationships, several nucleoside and base analogues were synthesized and 2'-deoxy-2-(p-nitrophenyl)-adenosine (8) was the most potent mutagen as tested either with TA 98 or TA 100.