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Molecules 2011, 16(9), 7649-7661; doi:10.3390/molecules16097649

Synthesis of Quinolin-2-one Alkaloid Derivatives and Their Inhibitory Activities against HIV-1 Reverse Transcriptase

1,3,* , 2
1 National Research Center of Engineering Technology For Utilization of Functional Ingredients From Botanicals, College of Horticulture and Landscape Architecture, Hunan Agricultural University, Changsha 410128, Hunan, China 2 School of Pharmaceutical Sciences, Sun Yat-Sen University, Guangzhou 510006, Guangdong,China 3 Hunan Engineering Research Center of Botanical Extract, Changsha410128, Hunan, China
* Authors to whom correspondence should be addressed.
Received: 16 June 2011 / Revised: 4 August 2011 / Accepted: 20 August 2011 / Published: 7 September 2011
(This article belongs to the Special Issue Antivirals)
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Based on an established common pharmacophore of HIV-1 non-nucleoside reverse transcriptase inhibitors (NNTTIs), a series of quinolin-2-one derivatives were synthesized and assayed for their in vitro activities against HIV-1 reverse transcriptase (RT) for the first time. Some of the tested compounds were active against HIV-1 RT. Compounds 4a2 and 4d2 showed inhibitory activities with IC50 values of 0.21 and 0.15 mM, respectively, with a mode of interaction with RT residues of the allosteric pocket similar to that of efavirenz.
Keywords: quinolin-2-one; alkaloid; synthesis; HIV-1 RT; activity quinolin-2-one; alkaloid; synthesis; HIV-1 RT; activity
This is an open access article distributed under the Creative Commons Attribution License (CC BY) which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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Cheng, P.; Gu, Q.; Liu, W.; Zou, J.-F.; Ou, Y.-Y.; Luo, Z.-Y.; Zeng, J.-G. Synthesis of Quinolin-2-one Alkaloid Derivatives and Their Inhibitory Activities against HIV-1 Reverse Transcriptase. Molecules 2011, 16, 7649-7661.

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