The potency and selectivity index of the AZT-phenyl phosphate derivatives in thymidine kinase (TK)-deficient T cells were substantially enhanced by introducing a single para-bromo substituent in the phenyl moiety. AZT-5′-(p-bromophenyl methoxyalaninyl phosphate) was 43-fold more potent than AZT-5′-(phenyl methoxyalaninyl phosphate) and was fivefold more potent than AZT in inhibiting human immunodeficiency virus (HIV) replication in TK-deficient CEM cells.
Antiviral Chemistry and Chemotherapy – SAGE
Published: Jun 23, 2016
Keywords: AZT derivatives,HIV,thymidine kinase-deficient T cells