944547-30-2Relevant articles and documents
Synthesis, structural studies and antitumoral evaluation of C-6 alkyl and alkenyl side chain pyrimidine derivatives
Kristafor, Svjetlana,Kraljevic, Tatjana Gazivoda,Makuc, Damjan,Plavec, Janez,Suman, Lidija,Kralj, Marijeta,Raic-Malic, Silvana
scheme or table, p. 4866 - 4879 (2010/04/05)
The synthetic route for introduction of fluorophenylalkyl (compounds 5, 7, 14 and 15) and fluorophenylalkenyl (compounds 4E and 13) side chains at C-6 of the pyrimidine nucleus involved the lithiation of the pyrimidine derivatives 1, 2 and 11 and subseque
Discovery of 5-substituted-6-chlorouracils as efficient inhibitors of human thymidine phosphorylase
Nencka, Radim,Votruba, Ivan,H?ebabecky, Hubert,Jansa, Petr,Tlou?t'ová, Eva,Horská, Květa,Masojídková, Milena,Holy, Antonín
, p. 6016 - 6023 (2008/09/17)
Thymidine phosphorylase plays an important role in angiogenesis, which is an attractive target for therapy of cancer and other diseases. In our continuous effort to develop novel inhibitors of thymidine phosphorylase, we have discovered that 6-halouracils substituted at position C5 by certain hydrophobic groups exhibit significant inhibitory activity against this enzyme. The most potent compounds bear a five- or six-membered cyclic substituent containing a π-electron system at C5 and a chlorine atom attached at C6. 6-Chloro-5-cyclopent-1-en-1-yluracil 7a is the most efficient derivative in this study, with Ki = 0.20 ± 0.03 μM (Ki/ dThdKm = 0.0017) for thymidine phosphorylase expressed in V79 cells and Ki = 0.29 ± 0.04 μM (Ki/ dThdKm = 0.0024) for the enzyme purified from placenta.
