Design and Synthesis of a Series of Truncated Neplanocin Fleximers
AbstractIn an effort to study the effects of flexibility on enzyme recognition and activity, we have developed several different series of flexible nucleoside analogues in which the purine base is split into its respective imidazole and pyrimidine components. The focus of this particular study was to synthesize the truncated neplanocin A fleximers to investigate their potential anti-protozoan activities by inhibition of S-adenosylhomocysteine hydrolase (SAHase). The three fleximers tested displayed poor anti-trypanocidal activities, with EC50 values around 200 μM. Further studies of the corresponding ribose fleximers, most closely related to the natural nucleoside substrates, revealed low affinity for the known T. brucei nucleoside transporters P1 and P2, which may be the reason for the lack of trypanocidal activity observed. View Full-Text
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Zimmermann, S.C.; O'Neill, E.; Ebiloma, G.U.; Wallace, L.J.M.; De Koning, H.P.; Seley-Radtke, K.L. Design and Synthesis of a Series of Truncated Neplanocin Fleximers. Molecules 2014, 19, 21200-21214.
Zimmermann SC, O'Neill E, Ebiloma GU, Wallace LJM, De Koning HP, Seley-Radtke KL. Design and Synthesis of a Series of Truncated Neplanocin Fleximers. Molecules. 2014; 19(12):21200-21214.Chicago/Turabian Style
Zimmermann, Sarah C.; O'Neill, Elizaveta; Ebiloma, Godwin U.; Wallace, Lynsey J.M.; De Koning, Harry P.; Seley-Radtke, Katherine L. 2014. "Design and Synthesis of a Series of Truncated Neplanocin Fleximers." Molecules 19, no. 12: 21200-21214.