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Synthesis and Evaluation of Aryl Quinolines as HIV-1 Integrase Multimerization Inhibitors.

ABSTRACT: HIV-1 integrase multimerization inhibitors have recently been established as an effective class of antiretroviral agents due to their potent ability to inhibit viral replication. Specifically, quinoline-based inhibitors have been shown to effectively impair HIV-1 replication, highlighting the importance of these heterocyclic scaffolds. Pursuant of our endeavors to further develop a library of quinoline-based candidates, we have implemented a structure-activity relationship study of trisubstituted 4-arylquinoline scaffolds that examined the integrase multimerization properties of substitution patterns at the 4-position of the quinoline. Compounds consisting of substituted phenyl rings, heteroaromatics, or polycyclic moieties were examined utilizing an integrase aberrant multimerization in vitro assay. para-Chloro-4-phenylquinoline 11b and 2,3-benzo[b][1,4]dioxine 15f showed noteworthy EC50 values of 0.10 and 0.08 ?M, respectively.

SUBMITTER: Jentsch NG 

PROVIDER: S-EPMC6187413 | biostudies-literature | 2018 Oct

REPOSITORIES: biostudies-literature

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Synthesis and Evaluation of Aryl Quinolines as HIV-1 Integrase Multimerization Inhibitors.

Jentsch Nicholas G NG   Hart Alison P AP   Hume Jared D JD   Sun Jian J   McNeely Kaitlin A KA   Lama Chiyang C   Pigza Julie A JA   Donahue Matthew G MG   Kessl Jacques J JJ  

ACS medicinal chemistry letters 20180914 10

HIV-1 integrase multimerization inhibitors have recently been established as an effective class of antiretroviral agents due to their potent ability to inhibit viral replication. Specifically, quinoline-based inhibitors have been shown to effectively impair HIV-1 replication, highlighting the importance of these heterocyclic scaffolds. Pursuant of our endeavors to further develop a library of quinoline-based candidates, we have implemented a structure-activity relationship study of trisubstitute  ...[more]

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