عنوان المقالة:Exploration of the in vitro anti-HIV and cyclin-dependent kinase 2 (CDK2) inhibitory activities of new 6-aryl-pyrimidines and their nitroso analogues
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-nu-
cleoside 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 IC
50
value of 1.83 μΜ 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 ad-
dition, the CDK2 inhibitory activity of the 5-nitrosopyrimidine analogues 23-27 and 35-38 was evaluated.
أ. د ناظر نجم عبدالله الكطراني | Nadhir Najim Abdullah Jafar | 4580