Indolylarylsulfones bearing phenylboronic acid and phenylboronate ester functionalities as potent HIV­1 non-nucleoside reverse transcriptase inhibitors.

Xu, Shujing; Song, Shu; Sun, Lin; Gao, Ping; Gao, Shenghua; Ma, Yue; Kang, Dongwei; Cheng, Yusen; Zhang, Xujie; Cherukupalli, Srinivasulu; De Clercq, Erik; Pannecouque, Christophe; Liu, Xinyong; Zhan, Peng

Indolylarylsulfones bearing phenylboronic acid and phenylboronate ester functionalities as potent HIV1 non-nucleoside reverse transcriptase inhibitors.

Xu, Shujing; Song, Shu; Sun, Lin; Gao, Ping; Gao, Shenghua; Ma, Yue; Kang, Dongwei; Cheng, Yusen; Zhang, Xujie; Cherukupalli, Srinivasulu; De Clercq, Erik; Pannecouque, Christophe; Liu, Xinyong; Zhan, Peng.

Afiliación

Xu S; Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Cheeloo College of Medicine, Shandong University, 44 West Culture Road, 250012 Jinan, Shandong, PR China.
Song S; Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Cheeloo College of Medicine, Shandong University, 44 West Culture Road, 250012 Jinan, Shandong, PR China.
Sun L; Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Cheeloo College of Medicine, Shandong University, 44 West Culture Road, 250012 Jinan, Shandong, PR China.
Gao P; Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Cheeloo College of Medicine, Shandong University, 44 West Culture Road, 250012 Jinan, Shandong, PR China.
Gao S; Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Cheeloo College of Medicine, Shandong University, 44 West Culture Road, 250012 Jinan, Shandong, PR China.
Ma Y; Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Cheeloo College of Medicine, Shandong University, 44 West Culture Road, 250012 Jinan, Shandong, PR China.
Kang D; Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Cheeloo College of Medicine, Shandong University, 44 West Culture Road, 250012 Jinan, Shandong, PR China.
Cheng Y; Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Cheeloo College of Medicine, Shandong University, 44 West Culture Road, 250012 Jinan, Shandong, PR China.
Zhang X; Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Cheeloo College of Medicine, Shandong University, 44 West Culture Road, 250012 Jinan, Shandong, PR China.
Cherukupalli S; Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Cheeloo College of Medicine, Shandong University, 44 West Culture Road, 250012 Jinan, Shandong, PR China.
De Clercq E; Rega Institute for Medical Research, Laboratory of Virology and Chemotherapy, K.U. Leuven, Herestraat 49 Postbus 1043 (09.A097), B-3000 Leuven, Belgium.
Pannecouque C; Rega Institute for Medical Research, Laboratory of Virology and Chemotherapy, K.U. Leuven, Herestraat 49 Postbus 1043 (09.A097), B-3000 Leuven, Belgium. Electronic address: christophe.pannecouque@kuleuven.be.
Liu X; Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Cheeloo College of Medicine, Shandong University, 44 West Culture Road, 250012 Jinan, Shandong, PR China; China-Belgium Collaborative Research Center for Innovative Antiv
Zhan P; Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Cheeloo College of Medicine, Shandong University, 44 West Culture Road, 250012 Jinan, Shandong, PR China; China-Belgium Collaborative Research Center for Innovative Antiv

Bioorg Med Chem ; 53: 116531, 2022 01 01.

Article en En | MEDLINE | ID: mdl-34890994

Asunto(s)

Fármacos Anti-VIH/farmacología; Ácidos Borónicos/farmacología; Ésteres/farmacología; Indoles/farmacología; Inhibidores de la Transcriptasa Inversa/farmacología; Sulfonas/farmacología; Fármacos Anti-VIH/síntesis química; Fármacos Anti-VIH/química; Ácidos Borónicos/química; Relación Dosis-Respuesta a Droga; Ésteres/química; Transcriptasa Inversa del VIH/antagonistas & inhibidores; Transcriptasa Inversa del VIH/metabolismo; VIH-1/efectos de los fármacos; VIH-1/enzimología; Indoles/química; Pruebas de Sensibilidad Microbiana; Modelos Moleculares; Estructura Molecular; Inhibidores de la Transcriptasa Inversa/síntesis química; Inhibidores de la Transcriptasa Inversa/química; Solubilidad; Relación Estructura-Actividad; Sulfonas/química; Agua/química

Palabras clave

Boronic acid; HIV-1; Indole-2-carboxamide; NNRTIs; SARs

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Texto completo: 1 Banco de datos: MEDLINE Asunto principal: Sulfonas / Ácidos Borónicos / Inhibidores de la Transcriptasa Inversa / Fármacos Anti-VIH / Ésteres / Indoles Idioma: En Revista: Bioorg Med Chem Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2022 Tipo del documento: Article

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