carbocyclic inosine (cas 16975-94-3) as a potent anti-Leishmanial agent: The metabolism and selective cytotoxic effects of carbocyclic inosine (cas 16975-94-3) in promastigotes of Leishmania tropica

Add time:08/05/2019    Source:sciencedirect.com

carbocyclic inosine (cas 16975-94-3) is a potent inhibitor for the growth of the promastigote form of Leishmania tropica and Leishmania donovani. In culture, the EC50 values of carbocyclic inosine are 8.3 × 10−8 and 1.3 × 10−7M for the promastigotes of L. tropica and L. donovani, respectively. On the other hand, it is less toxic towards mouse mammary tumor FM3A cells: the EC50 value is 2.7 × 10−4M. Carbocyclic inosine is metabolized by Leishmania promastigotes to give carbocyclic adenosine-5′-triphosphate (aristeromycin-5′-triphosphate) and carbocyclic guanosine-5′-triphosphate. This metabolic conversion provides a mechanism for the parasite-selective toxicity of carbocyclic inosine.

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