| Autor: |
Al-Masoudi, Najim A., Saeed, Bahjat A., Ali, Dawood S., Alias, Rita S., Jaffer, Nadhir N. A., Pannecouque, Christophe |
| Předmět: |
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| Zdroj: |
Chemistry & Biology Interface; Jan/Feb2016, Vol. 6 Issue 1, p1-13, 13p |
| Abstrakt: |
A new series of 2-amino-4-benzyloxy-6-(2-fluorophenyl)pyrimidine derivatives (14-22) were synthesized via Suzuki-Miyaura cross-coupling reaction, with the aim of developing novel HIV non-nucleoside reverse transcriptase inhibitors. All the synthesized compounds were structurally confirmed by spectral analyses. The compounds were evaluated for their antiviral activity against the replication of HIV-1 and HIV-2 in MT-4 cells using an MTT assay. Compound 20 exhibited IC50 value of 1.83 µ? with SI = 10.3 against HIV-1. In a docking study, 20 interacted with several amino acids in the reverse transcriptase (RT) binding site of HIV-1, and the results suggest that 20 can be considered as a new lead in the development of antiviral agents. The structure activity relationship (SAR) of these new analogues was studied as well. In addition, the CDK2 inhibitory activity of the 5-nitrosopyrimidine analogues 23-27 and 35-38 was evaluated. [ABSTRACT FROM AUTHOR] |
| Databáze: |
Complementary Index |
| Externí odkaz: |
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