Ontology highlight
ABSTRACT:
SUBMITTER: Dang Z
PROVIDER: S-EPMC4789664 | biostudies-literature | 2016 Mar
REPOSITORIES: biostudies-literature
Dang Zhao Z Zhu Lei L Lai Weihong W Bogerd Hal H Lee Kuo-Hsiung KH Huang Li L Chen Chin-Ho CH
ACS medicinal chemistry letters 20160109 3
A quinolizidine-type alkaloid aloperine was found to inhibit HIV-1 infection by blocking HIV-1 entry. Aloperine inhibited HIV-1 envelope-mediated cell-cell fusion at low micromolar concentrations. To further improve the antiviral potency, more than 30 aloperine derivatives with a variety of N12-substitutions were synthesized. Among them, 12d with an N-(1-butyl)-4-trifluoromethoxy-benzamide side chain showed the most potent anti-HIV-1 activity with EC50 at 0.69 μM. Aloperine derivatives inhibited ...[more]