Publication:
Synthesis, in vitro evaluation, and docking studies of novel chromone derivatives as HIV-1 protease inhibitor

Issued Date

2011-08-24

Resource Type

Article

ISSN

00222860

DOI

10.1016/j.molstruc.2011.06.035

Other identifier(s)

2-s2.0-79961032360

Rights

Mahidol University

Rights Holder(s)

SCOPUS

Bibliographic Citation

Journal of Molecular Structure. Vol.1001, No.1-3 (2011), 152-161

Suggested Citation

Jiraporn Ungwitayatorn, Chanpen Wiwat, Weerasak Samee, Patcharawee Nunthanavanit, Narumol Phosrithong Synthesis, in vitro evaluation, and docking studies of novel chromone derivatives as HIV-1 protease inhibitor. Journal of Molecular Structure. Vol.1001, No.1-3 (2011), 152-161. doi:10.1016/j.molstruc.2011.06.035 Retrieved from: https://repository.li.mahidol.ac.th/handle/123456789/11702

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Title

Synthesis, in vitro evaluation, and docking studies of novel chromone derivatives as HIV-1 protease inhibitor

Author(s)

Jiraporn Ungwitayatorn
 Chanpen Wiwat
 Weerasak Samee
 Patcharawee Nunthanavanit
 Narumol Phosrithong

Other Contributor(s)

Mahidol University
 Srinakharinwirot University
 Siam University

Abstract

Novel chromone derivatives with a benzopyran-4-one scaffold have been prepared by the one-pot cyclization reaction. The in vitro inhibitory activity of these new compounds towards HIV-1 protease have been evaluated using stop time HPLC method as the preliminary screening. The most potent compound, 7,8-dihydroxy-2-(3′-trifluoromethyl phenyl)-3-(3″- trifluoromethylbenzoyl)chromone (32), showed IC 50 = 0.34 μM. The molecular docking study supported results from experimental activity testing and also provided structure-activity relationship of this series. © 2011 Elsevier B.V. All rights reserved.

Keyword(s)

Chemistry

Availability

URI

https://repository.li.mahidol.ac.th/handle/123456789/11702

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Scopus 2011-2015