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

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

1,3,* , 2
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Received: 16 June 2011; in revised form: 4 August 2011 / Accepted: 20 August 2011 / Published: 7 September 2011
(This article belongs to the Special Issue Antivirals)
Download PDF [592 KB, updated 18 June 2014; original version uploaded 18 June 2014]
Abstract: 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 which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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MDPI and ACS Style

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.

AMA Style

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(9):7649-7661.

Chicago/Turabian Style

Cheng, Pi; Gu, Qiong; Liu, Wei; Zou, Jian-Feng; Ou, Yang-Yong; Luo, Zhong-Yong; Zeng, Jian-Guo. 2011. "Synthesis of Quinolin-2-one Alkaloid Derivatives and Their Inhibitory Activities against HIV-1 Reverse Transcriptase." Molecules 16, no. 9: 7649-7661.



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