Biochemical effects of 2′-fluoro-5-methyl-1-β-D-arabinofuranosyluracil and 2′-fluoro-5-iodo-1-β-D-arabinofuranosylcytosine in mouse leukemic cells sensitive and resistant to 1-β-D-arabinofuranosylcytosine was written by Chou, Ting Chao; Burchenal, Joseph H.; Schmid, Franz A.; Braun, Thomas J.; Su, Tsann Long; Watanabe, Kyoichi A.; Fox, Jack J.; Philips, Frederick S.. And the article was included in Cancer Research on October 31,1982.Recommanded Product: 69256-17-3 The following contents are mentioned in the article:
2′-fluoro-5-methyl-1-β-D-arabinofuranosyluracil (FMAU)(I) [69256-17-3], like 2′-fluoro-5-iodo-1-β-D-arabinofuranosylcytosine (FIAC)(II) [69123-90-6], has potent antiviral activity, but unlike FIAC, it also has antileukemic effects. The 2 agents and 1-β-D-arabinofuranosylcytosine (ara-C) [147-94-4] are compared herein. Concentrations inhibiting thymidine (dThd) incorporation into DNA by 50% are for FMAU, FIAC, and ara-C, resp., in L1210/0, 32, 353, and 0.2 μm and in L1210/ara-C, 17, <10,000, and 3900 μM. Other FMAU analogs, 2'-fluoro-5-ethyl-1-β-D-arabinofuranosyluracil [69123-98-4], inhibit dThd incorporation equally in ara-C-sensitive and -resistant cells; however, their potencies are weaker than that of FMAU. Similar results are obtained when [3H]deoxyadenosine is used as a precursor of incorporation. In L1210/0 cells, incorporation of [2-14C]FMAU radioactivity into DNA is completely inhibited by dThd and deoxycytidine (dCyd), whereas the incorporation of [2-14C]FIAC radioactivity is competitively inhibited by dCyd but not appreciably by dThd. In L1210/0 cells, FMAU has little inhibitory effect on the tritium release from [5-3H]deoxyuridine but markedly inhibits the incorporation of [2-14C]deoxyuridine into DNA. FIAC, by contrast, predominately inhibits the release of tritium from [5-3H]deoxyuridine but has little effect on subsequent incorporation into DNA. Apparently, (1) FIAC, but not FMAU, is cross-resistant to ara-C; (2) FMAU is particularly effective against L1210/ara-C cells; (3) FIAC behaves metabolically like dCyd, and FMAU like dThd and dCyd; (4) dCyd and dThd may be used as chemotherapeutic modulators; and (5) FIAC predominately inhibits dThd kinase and(or) thymidine monophosphate synthetase, whereas FMAU predominately inhibits DNA polymerase and(or) nucleotide kinases. Similar conclusions were obtained when P815/0 and P815/ara-C cells were used. The relative potencies of FIAC and FMAU in inhibiting dThd incorporation into DNA in leukemic sublines correlate with cytotoxicity in vitro and chemotherapeutic effects in vivo. This study involved multiple reactions and reactants, such as 1-((2R,3S,4R,5R)-3-Fluoro-4-hydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl)-5-methylpyrimidine-2,4(1H,3H)-dione (cas: 69256-17-3Recommanded Product: 69256-17-3).
1-((2R,3S,4R,5R)-3-Fluoro-4-hydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl)-5-methylpyrimidine-2,4(1H,3H)-dione (cas: 69256-17-3) belongs to pyrimidine derivatives. Heterocyclic compounds bearing the pyrimidine core are of tremendous interest as they constitute an important class of natural and synthetic compounds exhibiting diverse useful biological activities that hold attractive potential for clinical translation as therapeutic agents in alleviation of a myriad of diseases. Pyrimidine derivatives have been used in a wide variety of pharmaceuticals including general anesthetics, anti-epilepsy medication, anti-malaria medication, drugs for treating high blood pressure, and HIV medication.Recommanded Product: 69256-17-3
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