From:  Natural pentafuranosylnucleos(t)ides and their analogs: structure, functions, synthesis, and perspective of medical application

 Inhibition of human recombinant poly(adenosine diphosphate ribose) polymerase (PARP)-1 by some synthetic nucleoside analogs with different carbohydrate moiety

Carbohydrate moietyCompoundBaseModificationIC50 µM
52AdeMe2'-O-α-D-Ara (53)93.4 ± 3.7
53AdeMe> 250
54AdeiPr2'-O-α-D-Ara (55)158.2 ± 17.7
55AdeiPr> 250
56PurOMe2'-O-α-D-Ara> 250
57PurOMe
58PurSH2'-O-α-D-Ara> 250
59PurSH
60PurSMe2'-O-α-D-Ara> 250
61PurSMe
62Thy178 ± 6
63aUra5-F45 ± 3
63bUra5-I38 ± 4
63cThy5'-PO3H> 2,000
63dThy5''-PO3H216 ± 56
3'-Rib-α-Thd64Thy> 2,000
65Thy25 ± 3
3-Amino benzamide57 ± 8

Thd: thymidine; AdeMe: N6-methyladenine; AdeiPr: N6-isopropyladenine; PurOMe: 6-methoxypurine; PurSH: 6-thiopurine; PurSMe: 6-methylthiopurine; Thy: thymine; Ura: uracil; Ara: arabinofuranose; IC50: half maximal concentration, at which 50% enzymatic activity reduction is observed