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Synthesis of quinolin-2-one alkaloid derivatives and their inhibitory activities against HIV-1 reverse transcriptase.

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 IC(50) 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.

SUBMITTER: Cheng P 

PROVIDER: S-EPMC6264335 | biostudies-literature | 2011 Sep

REPOSITORIES: biostudies-literature

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Synthesis of quinolin-2-one alkaloid derivatives and their inhibitory activities against HIV-1 reverse transcriptase.

Cheng Pi P   Gu Qiong Q   Liu Wei W   Zou Jian-Feng JF   Ou Yang-Yong YY   Luo Zhong-Yong ZY   Zeng Jian-Guo JG  

Molecules (Basel, Switzerland) 20110907 9

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 IC(50) values of 0.21 and 0.15 mM, respectively, with a mode of interaction with RT residues of the allosteric poc  ...[more]

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