Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 186, Issue -, Pages -Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2019.111900
Keywords
Coumarin; HIV-1 PR inhibitors; HIV-1 RT inhibitors; Pharmacophore fusion types
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Funding
- National Natural Science Foundation of China [81703366]
- CAMS Innovation Fund for Medical Sciences [CIFMS 2016-I2M-1-011, 2018-I2M-3-004]
- National Mega-Project for Infectious Disease [2018ZX10301408]
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Since dual inhibitors may yield lower toxicity and reduce the likelihood of drug resistance, as well as inhibitors of HIV-1 PR and RT constitute the core of chemotherapy for AIDS treatment, we herein designed and synthesized new coumarin derivatives characterized by various linkers that exhibited excellent potency against PR and a weak inhibition of RT. Among which, compounds 6f and 7c inhibited PR with IC50 values of 15.5 and 62.1 nM, respectively, and weakly affected also RT with IC50 values of 241.8 and 188.7 mu M, respectively, showing the possibility in the future of developing dual HIV-1 PR/RT inhibitors. Creative stimulation for further research of more potent dual HIV-1 inhibitors was got according to the molecular docking studies. (C) 2019 Elsevier Masson SAS. All rights reserved.
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