Antiretroviral activity and cytotoxicity of novel zidovudine (AZT) derivatives and the relation to their chemical structure
- Turk, Gabriela Julia Ana
- Fernández Moroni, Guillermo
- Pampuro, Sandra Esther
- Brión, Margarita C.
- Salomon, Horacio Eduardo
DOIAbstract
Zidovudine (AZT) was the first nucleoside analogue licensed for the treatment of HIV infection. Efforts have continuously been made to improve the therapeutic characteristics of this drug, most of them focussed on prodrugs design. Here we describe the anti-HIV-1 activity and cytotoxicity of six novel AZT derivatives namely 3′-azido-3′-deoxy-5′-O-oxalyl-N-valinethymidine, 3′-azido-3′-deoxy-5′-O-oxalyl-N-leucinethymidine, 3′-azido-3′-deoxy-5′-O-oxalyl-N-isoleucinethymidine, 3′-azido-3′-deoxy-5′-O-oxalyl-N-phenylalaninethymidine, 3′-azido-3′-deoxy-5′-O-oxalylthymidine acid, 3′-azido-3′-deoxy-5′-O-isonicotinoylthymidine and 5-chloro-6-hydroxy-5,6-dihydro-3′-azido-3′-deoxythymidine which were perfectly characterized. AZT-Val, AZT-Leu, AZT-iLeu, ...
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