- Synthesis and antiviral activity of lycorine derivatives
-
There are no effective antiviral drugs to treat hand, foot, and mouth disease. In this study, a series of lycorine derivatives were synthesized and evaluated against enterovirus 71 and coxsackievirus A16 in?vitro. Derivatives 7c-m with the phenoxyacyl gro
- Yang, Ya-Jun,Liu, Jiang-Ning,Pan, Xian-Dao
-
p. 1188 - 1196
(2020/11/19)
-
- Preparation of Structurally Diverse Compounds from the Natural Product Lycorine
-
The synthesis of a 52-member compound collection from the natural product lycorine is reported, highlighted by divergent cross-coupling and substitution strategies and an unusual ring rearrangement induced by reaction with aryne intermediates.
- Tasker, Sarah Z.,Cowfer, Amanda E.,Hergenrother, Paul J.
-
p. 5894 - 5898
(2018/09/25)
-
- Lycorine derivatives and application thereof to pesticides
-
The invention relates to lycorine compounds with structures from (1-1) to (1-20) represented in the description as well as an application of the lycorine compounds to pesticides. When the lycorine compounds are used as novel insecticides and bactericides, part of the compounds have toxic activity on armyworms, mosquito larvae, cotton bollworms and ostrinia nubilalis and have higher inhibition ratio on wheat scab, potato late blight, rape sclerotinia rot and cucumber gray mold than that of a lycorine matrix.
- -
-
Paragraph 0040-0042
(2017/11/16)
-
- Lycorine alkali compound in preparing an anti-tumor drug application
-
The invention relates to application of a Lycorine compound in anti-tumor drugs, and also relates to application of its various optical isomers, pharmaceutically acceptable salts, solvates and prodrugs in preparation of anti-tumor drugs. The invention also relates to application of pharmaceutical compositions containing the Lycorine compound with a structure shown as formula (A) in preparation of anti-tumor drugs.
- -
-
-
- Anti-dengue-virus activity and structure-activity relationship studies of lycorine derivatives
-
Dengue is a systemic viral infection that is transmitted to humans by Aedes mosquitoes. No vaccines or specific therapeutics are currently available for dengue. Lycorine, which is a natural plant alkaloid, has been shown to possess antiviral activities against flaviviruses. In this study, a series of novel lycorine derivatives were synthesized and assayed for their inhibition of dengue virus (DENV) in cell cultures. Among the lycorine analogues, 1-acetyllycorine exhibited the most potent anti-DENV activity (EC50=0.4 μM) with a reduced cytotoxicity (CC50>300 μM), which resulted in a selectivity index (CC50/EC50) of more than 750. The ketones 1-acetyl-2-oxolycorine (EC50=1.8 μM) and 2-oxolycorine (EC50=0.5 μM) also exhibited excellent antiviral activities with low cytotoxicity. Structure-activity relationships for the lycorine derivatives against DENV are discussed. A three-dimensional quantitative structure-activity relationship model was established by using a comparative molecular-field analysis protocol in order to rationalize the experimental results. Further modifications of the hydroxy group at the C1 position with retention of a ketone at the C2 position could potentially lead to inhibitors with improved overall properties. Alkaloids that bite back: Dengue is a systemic viral infection that is transmitted to humans by Aedes mosquitoes. Currently, vaccines or specific therapeutics are not available. Lycorine, which is a natural alkaloid, has reportedly demonstrated biological activity against dengue virus (DENV). A series of lycorine derivatives and their anti-DENV activities are reported herein.
- Wang, Peng,Li, Lin-Feng,Wang, Qing-Yin,Shang, Lu-Qing,Shi, Pei-Yong,Yin, Zheng
-
p. 1522 - 1533
(2014/07/21)
-