82276-89-9Relevant academic research and scientific papers
Synthesis and in Vivo Antitumor Activity of Potential 5-Fluorouracil Prodrugs
Rosowsky, A.,Kim, S.-H.,Trites, D.,Wick, M.
, p. 1034 - 1040 (1982)
Analogues of 5'-deoxy-5-fluorouridine (DFUR, 1) were synthesized with the aim of evaluating the effect of structural modification of the 5' region of the ribofuranose moiety on the activity of these potential prodrug derivatives of 5-fluorouracil (FU).Rea
Synthesis and structure-activity relationship of uracil nucleotide derivatives towards the identification of human P2Y6 receptor antagonists
Meltzer, Diana,Ethan, Ophir,Arguin, Guillaume,Nadel, Yael,Danino, Ortal,Lecka, Joanna,Sévigny, Jean,Gendron, Fernand-Pierre,Fischer, Bilha
, p. 5764 - 5773 (2015/11/11)
P2Y6 receptor (P2Y6-R) is involved in various physiological and pathophysiological events. With a view to set rules for the design of UDP-based reversible P2Y6-R antagonists as potential drugs, we established structure-activity relationship of UDP analogues, bearing modifications at the uracil ring, ribose moiety, and the phosphate chain. For instance, C5-phenyl- or 3-NMe-uridine-5′-α,β-methylene-diphosphonate, 16 and 23, or lack of 2′-OH, in 12-15, resulted in loss of both agonist and antagonist activity toward hP2Y6-R. However, uridylyl phosphosulfate, 19, selectively inhibited hP2Y6-R (IC50 112 μM) versus P2Y2/4-Rs. In summary, we have established a comprehensive SAR for hP2Y6-R ligands towards the development of hP2Y6-R antagonists.
Porphyrinyl-nucleosides containing fluorinated nucleobases
Czuchajowski,Palka,Morra,Wandrekar
, p. 5409 - 5412 (2007/10/02)
Porphyrins were synthesized in which a meso-p-phenylene-O-bridge joins the porphine core with 5'-C of 5-fluorouridine (protected), 5-CF3-thymidine or 2-N-trifluoroacetamidato-6-O-pentafluorophenyl-2'-deoxyguanosine.
