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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 3.0).

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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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