Please use this identifier to cite or link to this item:
|Title:||Synthesis, structure-activity relationships, and mechanism of action of anti-HIV-1 lamellarin α 20-sulfate analogues||Authors:||Kamiyama, H.
Entry inhibiting activity
|Issue Date:||15-Dec-2011||Citation:||Kamiyama, H., Kubo, Y., Sato, H., Yamamoto, N., Fukuda, T., Ishibashi, F., Iwao, M. (2011-12-15). Synthesis, structure-activity relationships, and mechanism of action of anti-HIV-1 lamellarin α 20-sulfate analogues. Bioorganic and Medicinal Chemistry 19 (24) : 7541-7550. ScholarBank@NUS Repository. https://doi.org/10.1016/j.bmc.2011.10.030||Abstract:||Lamellarin α and six different types of lamellarin α 20-sulfate analogues were synthesized and their structure-activity relationships were investigated using a single round HIV-1 vector infection assay. All lamellarin sulfates having pentacyclic lamellarin core exhibited anti-HIV-1 activity at a 10 μM concentration range regardless of the number and position of the sulfate group. On the other hand, non-sulfated lamellarin α and ring-opened lamellarin sulfate analogues did not affect HIV-1 vector infection in similar concentrations. The lamellarin sulfates utilized in this study did not exhibit unfavorable cytotoxic effect under the concentrations tested (IC 50 > 100 μM). Confocal laser scanning microscopic analysis indicated that hydrophilic lamellarin sulfates were hardly incorporated in the cell. HIV-1 Env-mediated cell-cell fusion was suppressed by lamellarin sulfates. These results suggested that lamellarin sulfates have a novel anti-HIV-1 activity besides the previously reported integrase activity inhibition, possibly at a viral entry step of HIV-1 replication. © 2011 Elsevier Ltd. All rights reserved.||Source Title:||Bioorganic and Medicinal Chemistry||URI:||http://scholarbank.nus.edu.sg/handle/10635/126752||ISSN:||09680896||DOI:||10.1016/j.bmc.2011.10.030|
|Appears in Collections:||Staff Publications|
Show full item record
Files in This Item:
There are no files associated with this item.
checked on Aug 13, 2019
WEB OF SCIENCETM
checked on Aug 5, 2019
checked on Aug 16, 2019
Items in DSpace are protected by copyright, with all rights reserved, unless otherwise indicated.