78097-06-0

Upstream product

• 58305-05-8 (2-benzoyloxyethyl)oxymethyl chloride 
• 3444-09-5 1,3-bis(trimethylsilyl)thymine 
• 94-33-7 C₉H₁₀O₃ 
• 7288-28-0 2,4-bis(trimethylsiloxy)-5-methylpyrimidine 

Downstream Products

• 68724-11-8 1-[(2-hydroxyethoxy)methyl]thymine 
• 88070-48-8 N-methylbenzamide 

Relevant academic research and scientific papers

PREVENTION AND TREATMENT OF CANCER AND OTHER DISEASES

Nucleoside chemical compounds, which interact with specific structures of deoxyribonucleic acid (DNA) or ribonucleic acid (RNA) are disclosed. The compounds interfere with the activities of telomerase and reverse transcriptase, and are useful as antivirals, antibacterials and anticancer agents. Methods of treating or preventing cancers in patients involving administration of a therapeutically effective amount of a composition having an inhibitor or antagonist of the reverse transcriptases (RTs) expressed in cells of the patients are also disclosed. Method of using nucleoside analogs and other inhibitors of RTs in conjunction with DNA damaging agents such as genotoxic agents or radiation or photodynamic therapy or combinations these for the treatment of various cancers are also disclosed.

Synthesis and Biological Effects of Acyclic Pyrimidine Nucleoside Analogues

A series of nucleoside analogues has been prepared, wherein the cyclic carbohydrate moiety is replaced by aliphatic side chains attached to cytosine, thymine, uracil, and 5-fluorouracil.The 1- derivatives of these heterocycles were synthesized by reacting the silylated bases with 2-(chloromethoxy)ethyl benzoate, followed by removal of the protecting groups with methanolic ammonia.The hydroxy group of a number of these derivatives was subsequently replaced by an azido, amino, or carbamoyloxy moiety.The 1-(2-oxo-3-butyl) and 1-(2-oxo-3-nonyl)derivatives of cytosine were also prepared, their synthesis being accomplished by condensation of the silylated heterocycle with the appropriate α-halo ketone.At 10-4 M concentrations, the newly prepared compounds were inactive against leukemia L-1210 cells in culture.However, a number of the agents inhibited the in vitro growth of Escherichia coli K-12, the most potent among these, 1--5-fluorouracil, being active at an IC50 of 1.2 μM.This compound was equally active in preventing the growth of a 5-fluorouracil resistant strain of E. coli.Some of the analogues were also found the selectively interfere with herpes simplex virus replication in vitro.None of the cytosine derivatives tested served as either substrates or inhibitors of human liver citosine nucleoside deaminase.