Design, synthesis and biological activity evaluation of novel conjugated sialic acid and pentacyclic triterpene derivatives as anti-influenza entry inhibitors

MedChemComm ◽  
2016 ◽  
Vol 7 (10) ◽  
pp. 1932-1945 ◽  
Author(s):  
Xu Han ◽  
Yongying Shi ◽  
Longlong Si ◽  
Zibo Fan ◽  
Han Wang ◽  
...  
Keyword(s):  
Influenza Virus ◽  
Biological Activity ◽  
Sialic Acid ◽  
Virus Entry ◽  
Pentacyclic Triterpene ◽  
Design Synthesis ◽  
Entry Inhibitors ◽  
Activity Evaluation ◽  
Virus Entry Inhibitors

A total of 24 novel sialic acid–pentacyclic triterpene conjugates were synthesized and evaluated as anti-influenza virus entry inhibitors.

scholarly journals Synthesis of Four Pentacyclic Triterpene–Sialylglycopeptide Conjugates and Their Affinity Assays with Hemagglutinin

Molecules ◽  
2021 ◽  
Vol 26 (4) ◽  
pp. 895
Author(s):  
Mei Luo ◽  
Ximin Wu ◽  
Yiming Li ◽  
Fujiang Guo
Keyword(s):  
Influenza Virus ◽  
Virus Entry ◽  
Cycloaddition Reaction ◽  
Pentacyclic Triterpene ◽  
Entry Inhibitors ◽  
Important Target ◽  
Virus Entry Inhibitors ◽  
Influenza Outbreaks ◽  
Ha Protein ◽  
Dissociation Constant Kd

Influenza outbreaks pose a serious threat to human health. Hemagglutinin (HA) is an important target for influenza virus entry inhibitors. In this study, we synthesized four pentacyclic triterpene conjugates with a sialylglycopeptide scaffold through the Cu(I)-catalyzed alkyne-azide cycloaddition reaction (CuAAC) and prepared affinity assays of these conjugates with two HAs, namely H1N1 (A/WSN/1933) and H5N1 (A/Hong Kong/483/97), respectively. With a dissociation constant (KD) of 6.89 μM, SCT-Asn-betulinic acid exhibited the strongest affinity with the H1N1 protein. Furthermore, with a KD value of 9.10 μM, SCT-Asn-oleanolic acid exhibited the strongest affinity with the H5N1 protein. The conjugates considerably enhanced antiviral activity, which indicates that pentacyclic triterpenes can be used as a ligand to improve the anti-influenza ability of the sialylglycopeptide molecule by acting on the HA protein.

scholarly journals Reply to Padmanabhan and Dixit: Hepatitis C virus entry inhibitors for optimally boosting direct-acting antiviral-based treatments

2017 ◽  
Vol 114 (23) ◽  
pp. E4527-E4529 ◽  
Author(s):  
Hirofumi Ohashi ◽  
Yoshiki Koizumi ◽  
Kento Fukano ◽  
Takaji Wakita ◽  
Alan S. Perelson ◽  
...  
Keyword(s):  
Hepatitis C Virus ◽  
Hepatitis C ◽  
Virus Entry ◽  
Direct Acting Antiviral ◽  
Entry Inhibitors ◽  
Virus Entry Inhibitors ◽  
Direct Acting

scholarly journals Identification of Diaryl-Quinoline Compounds as Entry Inhibitors of Ebola Virus

Viruses ◽  
2018 ◽  
Vol 10 (12) ◽  
pp. 678 ◽  
Author(s):  
Qinghua Cui ◽  
Han Cheng ◽  
Rui Xiong ◽  
Gang Zhang ◽  
Ruikun Du ◽  
...  
Keyword(s):  
Drug Development ◽  
Ebola Virus ◽  
Virus Disease ◽  
Virus Entry ◽  
Surface Protein ◽  
Host Cells ◽  
Entry Inhibitor ◽  
Entry Inhibitors ◽  
Promising Target ◽  
Virus Entry Inhibitors

Ebola virus is the causative agent of Ebola virus disease in humans. The lethality of Ebola virus infection is about 50%, supporting the urgent need to develop anti-Ebola drugs. Glycoprotein (GP) is the only surface protein of the Ebola virus, which is functionally critical for the virus to attach and enter the host cells, and is a promising target for anti-Ebola virus drug development. In this study, using the recombinant HIV-1/Ebola pseudovirus platform we previously established, we evaluated a small molecule library containing various quinoline compounds for anti-Ebola virus entry inhibitors. Some of the quinoline compounds specifically inhibited the entry of the Ebola virus. Among them, compound SYL1712 was the most potent Ebola virus entry inhibitor with an IC50 of ~1 μM. The binding of SYL1712 to the vial glycoprotein was computationally modeled and was predicted to interact with specific residues of GP. We used the time of the addition assay to show that compound SYL1712 blocks Ebola GP-mediated entry. Finally, consistent with being an Ebola virus entry inhibitor, compound SYL1712 inhibited infectious Ebola virus replication in tissue culture under biosafety level 4 containment, with an IC50 of 2 μM. In conclusion, we identified several related molecules with a diaryl-quinoline scaffold as potential anti-EBOV entry inhibitors, which can be further optimized for anti-Ebola drug development.

Design, synthesis, and biological activity evaluation of (-)-6-O-desmethylantofine analogues as potent anti-cancer agents

2019 ◽  
Vol 27 (14) ◽  
pp. 3070-3081 ◽  
Author(s):  
Guifang Han ◽  
Lihua Qing ◽  
Meng Wu ◽  
Yuxiang Wang ◽  
Yuxiu Liu ◽  
...  
Keyword(s):  
Biological Activity ◽  
Design Synthesis ◽  
Activity Evaluation ◽  
Anti Cancer

scholarly journals Advancing hepatitis B virus entry inhibitors

2017 ◽  
Vol 66 (4) ◽  
pp. 677-679 ◽  
Author(s):  
Eloi R. Verrier ◽  
Catherine Schuster ◽  
Thomas F. Baumert
Keyword(s):  
Hepatitis B Virus ◽  
Hepatitis B ◽  
Virus Entry ◽  
Entry Inhibitors ◽  
B Virus ◽  
Virus Entry Inhibitors
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