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Molecules 2011, 16(9), 7649-7661;

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

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
School of Pharmaceutical Sciences, Sun Yat-Sen University, Guangzhou 510006, Guangdong,China
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. View Full-Text
Keywords: quinolin-2-one; alkaloid; synthesis; HIV-1 RT; activity quinolin-2-one; alkaloid; synthesis; HIV-1 RT; activity

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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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