Synthesis of 3-Deoxy-3-C-Trifluoromethyl-d-Ribose Fromd-Xylose ord-Glucose

Σύνθεση Μιας Νέας Τάξης Φθορο - Θειο - Νουκλεοζιτών Με Πιθανή Αντιϊκή Και Αντικαρκινική Δράση

“…On the contrary, thymine and uracil derivatives 19c,d showed no activity having EC 50 values higher than 100 [45]. Furthermore, it was found that in the -D-series, several purine derivatives, such as adenine 18d (EC 50 0.44 ) and hypoxanthine 18h (EC 50 1.0 ), showed significant antiviral activity, whereas in the -L-series the pyrimidine derivatives, cytosine 19a (EC 50 (Fig. 13) [46].…”

“…However, analogues 21a and 21b showed significantly decreased antiviral potency against the clinically important lamivudine-resistant variants (HIV-1 M184V ). The -guanosine analogue 21g showed only marginal anti-HIV activity with some cytotoxicity (EC 50 38.5 , and IC 50 17.4, 58.4, 36.5 , in PBM, CEM and Vero cells, respectively) [48]. Moreover, the D-cytosine and 5-fluoro-D-cytosine derivatives 20a and 20b were 100-to 500-fold less potent than their -L-isomers 21a and 21b [46].…”

“…Their anti-HIV-1 activity was evaluated in PBM cells, and the highest was found in the cytidine analogue 20a (EC 50 2.3 ). The adenine analogue 20e (EC 50 6.55 ), 5-fluorocytosine 20b (EC 50 9.29 ) and the hypoxanthine derivative 20f (EC 50 12.8 ) displayed moderate antiviral activity without significant cytotoxicity.…”

“…14) were described by Chen et al [49]. They tested these analogues for their antiviral properties against HIV in PBM cells in vitro and found that only the Dadenine derivative 22e showed moderate anti-HIV activity (EC 50 25.1 ) without any significant cytotoxicity.…”

“…The growth inhibition of Caco-2 cells induced by the new compounds was measured by determining the minimal inhibitory concentration (IC 50 ). The results are summarized in Table 2 and compared with the values obtained for 5FU.…”