Synthesis and in vitro anti-HIV-1 activity of a series of N-arylsulfonyl-3-propionylindoles
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Zhiping Che
Abstract
Fifteen N-arylsulfonyl-3-propionylindoles (3a–o) were prepared and preliminarily evaluated as in vitro inhibitors of human immunodeficiency virus type-1 (HIV-1). Three compounds 3c, 3g and 3i exhibited potent anti-HIV-1 activity with effective concentration (EC50) values of 0.8, 4.0 and 1.2 μg/mL, and therapeutic index (TI) values of 11.7, 16.6 and 84.1, respectively. N-(m-Nitro)phenylsulfonyl-3-propionyl-6-methylindole (3i) exhibited the most promising and best activity against HIV-1 replication. The cytotoxicity of these compounds was assessed as well.
Funding source: Henan University of Science and Technology
Award Identifier / Grant number: 2015GJB024
Award Identifier / Grant number: 09001763
Award Identifier / Grant number: 13580038
Funding statement: This work was financially supported by grants from the program for High Level Scientific Research Projects to Foster Funds of Henan University of Science and Technology (2015GJB024), the Doctoral Scientific Research Fund Project of Henan University of Science and Technology (09001763), and the Youth Science Foundation of Henan University of Science and Technology (13580038). We would like to acknowledge the MRC AIDS Research Project and the NIH AIDS Research and Reference Reagent Program for providing cell lines and viruses.
Acknowledgments:
This work was financially supported by grants from the program for High Level Scientific Research Projects to Foster Funds of Henan University of Science and Technology (2015GJB024), the Doctoral Scientific Research Fund Project of Henan University of Science and Technology (09001763), and the Youth Science Foundation of Henan University of Science and Technology (13580038). We would like to acknowledge the MRC AIDS Research Project and the NIH AIDS Research and Reference Reagent Program for providing cell lines and viruses.
Conflict of Interest: The authors have reported no conflict of interest.
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Articles in the same Issue
- Frontmatter
- Editorial
- ZNC opens a new chapter focussing on the emerging field of natural and natural-like compounds
- Research Articles
- Design, synthesis and evaluation of antitumor activity of new rotundic acid acylhydrazone derivatives
- Synthesis and in vitro anti-HIV-1 activity of a series of N-arylsulfonyl-3-propionylindoles
- Jaspiferin G, a new isomalabaricane-type triterpenoid from the sponge Jaspis stellifera
- The effect of coniine on presynaptic nicotinic receptors
- Nematicidal effect of plumbagin on Caenorhabditis elegans: a model for testing a nematicidal drug
- Synthesis and biological evaluation of novel pyrimidines derived from 6-aryl-5-cyano-2-thiouracil
- Phytochemical investigation of the bioactive extracts of the leaves of Ficus cyathistipula Warb.
- Chemical composition and biological activity of the essential oil from Thymus lanceolatus
- Ascidian bioresources: common and variant chemical compositions and exploitation strategy – examples of Halocynthia roretzi, Styela plicata, Ascidia sp. and Ciona intestinalis
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