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- W2952167519 abstract "Summary In order to prepare novel antiretroviral lead compounds active against human immunodeficiency virus type 1 reverse transcriptase (HIV-1 RT), a family of C-silylalkylated heterocyclic derivatives were synthesized. One of these derivatives 3 inhibited HIV-1 replication in cell culture (IC 50 = 12 ± 4 μM) without significant cytotoxic effects. This compound did not exhibit antiviral activity against herpes simplex virus type 1 and poliovirus type 1. Biochemical studies showed that 3 inhibited the DNA polymerase activity of a recombinant HIV-1 RT. This derivative was shown to be a non-competitive inhibitor with respect to dNTP substrate incorporation. Different levels of inhibition were obtained depending on the template-primer used. Compound 3 did not inhibit either the RNase H activity of HIV-1 RT, or the RNA-directed DNA polymerase activity of HIV-2 RT." @default.
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- W2952167519 date "1996-01-01" @default.
- W2952167519 modified "2023-10-18" @default.
- W2952167519 title "Novel C-organosilicon derivatives as leads for reverse-transcriptase-mediated anti-HIV-1 activity" @default.
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- W2952167519 doi "https://doi.org/10.1016/0223-5234(96)80444-2" @default.
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