9-deaza-9-(3-thienylmethyl)guanine has been researched along with deoxyguanosine-triphosphate* in 3 studies
3 other study(ies) available for 9-deaza-9-(3-thienylmethyl)guanine and deoxyguanosine-triphosphate
| Article | Year |
|---|---|
Apoptotic death induced in MOLT-4 T-lymphoblasts by purine nucleoside phosphorylase inhibition.
Topics: Apoptosis; Cell Line; Deoxyguanine Nucleotides; Deoxyguanosine; Enzyme Inhibitors; Guanine; Purine-Nucleoside Phosphorylase; T-Lymphocytes | 1997 |
Activities of two 9-deazaguanine analogue inhibitors of purine nucleoside phosphorylase, CI-972 and PD 141955, in vitro and in vivo.
Topics: Animals; Cell Division; Deoxyguanine Nucleotides; Dose-Response Relationship, Drug; Guanine; Humans; Immunosuppressive Agents; Purine-Nucleoside Phosphorylase; Pyrimidines; Rats; Thiophenes; Tumor Cells, Cultured | 1993 |
Comparative in vitro and in vivo activities of two 9-deazaguanine analog inhibitors of purine nucleoside phosphorylase, CI-972 and PD 141955.
An in-parallel comparison is presented of the in vitro and in vivo properties of two 9-deazaguanine analog inhibitors of purine nucleoside phosphorylase (PNP), CI-972 [8-amino-9-deaza-9-(3-thienylmethyl)guanine] and PD 141955 [9-deaza-9-(3-thienylmethyl)guanine] (published Ki values of 0.83-8.0 and 0.08 microM, respectively). Despite structural similarities, PD 141955 was considerably more potent and active in all systems studied. The respective IC50 values for inhibition of MOLT-4 cell growth in the absence and presence of 10 microM 2'-deoxyguanosine (GdR) were greater than 50 and 5.06 microM for CI-972 and 15.4 and 0.061 microM for PD 141955. PD 141955 induced accumulation of dGTP in GdR-treated MOLT-4 and CEM cells at log-lower concentrations than were required of CI-972, and the magnitude of dGTP accumulation in PD 141955-treated T cell cultures was markedly greater (e.g. 366 vs 100 pmol/10(6) CEM cells at 10 microM). PD 141955 administered orally produced a dose-dependent elevation of plasma inosine and guanosine in rats over a broad concentration range. Mean plasma inosine concentrations following a 150 mg/kg p.o. dose peaked at 6.21 and 13.2 microM in CI-972 and PD 141955-treated rats, respectively. Low levels of inosine were detectable at 50 micrograms/kg following oral administration of PD 141955. Topics: Animals; Cell Line; Deoxyguanine Nucleotides; Dose-Response Relationship, Drug; Guanine; Guanosine; Humans; Inosine; Male; Purine-Nucleoside Phosphorylase; Pyrimidines; Rats; Rats, Inbred Strains; T-Lymphocytes; Thiophenes | 1992 |