Abstract:
:Viral infectivity factor (Vif) is one of the accessory protein of human immunodeficiency virus type I (HIV-1) that inhibits host defense factor, APOBEC3G (A3G), mediated viral cDNA hypermutations. Previous work developed a novel Vif inhibitor 2-amino-N-(2-methoxyphenyl)-6-((4-nitrophenyl)thio)benzamide (1) with strong antiviral activity. Through optimizations on the two side branches, a series of compound 1 derivatives (2-18) were designed, synthesized and tested in vitro for their antiviral activities. The biological results showed that compound 5 and 16 inhibited the virus replication efficiently with EC50 values of 9.81 and 4.62 μM. Meanwhile, low cytotoxicities on H9 cells were observed for the generated compounds by the MTT assay. The structure-activity relationship of compound 1 was preliminarily clarified, which gave rise to the development of more potent Vif inhibitors.
journal_name
Bioorg Med Chem Lettjournal_title
Bioorganic & medicinal chemistry lettersauthors
Zhang RH,Wang S,Luo RH,Zhou M,Zhang H,Xu GB,Zhao YL,Li YJ,Wang YL,Yan G,Liao SG,Zheng YT,Li Rdoi
10.1016/j.bmcl.2019.126638subject
Has Abstractpub_date
2019-12-15 00:00:00pages
126638issue
24eissn
0960-894Xissn
1464-3405pii
S0960-894X(19)30583-9journal_volume
29pub_type
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