Application of the Morita-Baylis-Hillman reaction in the synthesis of 3-[(N-cycloalkylbenzamido)methyl]-2-quinolones as potential HIV-1 integrase inhibitors.

Sekgota, Khethobole C; Majumder, Swarup; Isaacs, Michelle; Mnkandhla, Dumisani; Hoppe, Heinrich C; Khanye, Setshaba D; Kriel, Frederik H; Coates, Judy; Kaye, Perry T

Sekgota, Khethobole C; Majumder, Swarup; Isaacs, Michelle; Mnkandhla, Dumisani; Hoppe, Heinrich C; Khanye, Setshaba D; Kriel, Frederik H; Coates, Judy; Kaye, Perry T.

Afiliação

Sekgota KC; Department of Chemistry, Rhodes University, Grahamstown 6140, South Africa.
Majumder S; Department of Chemistry, Rhodes University, Grahamstown 6140, South Africa.
Isaacs M; Centre for Chemico- and Biomedicinal Research, Rhodes University, Grahamstown 6140, South Africa.
Mnkandhla D; Centre for Chemico- and Biomedicinal Research, Rhodes University, Grahamstown 6140, South Africa.
Hoppe HC; Department of Biochemistry and Microbiology, Rhodes University, Grahamstown 6140, South Africa; Centre for Chemico- and Biomedicinal Research, Rhodes University, Grahamstown 6140, South Africa.
Khanye SD; Department of Chemistry, Rhodes University, Grahamstown 6140, South Africa; Centre for Chemico- and Biomedicinal Research, Rhodes University, Grahamstown 6140, South Africa.
Kriel FH; Centre for Metal-based Drug Discovery, Advanced Materials Division, Mintek, Randburg 2125, South Africa.
Coates J; Centre for Metal-based Drug Discovery, Advanced Materials Division, Mintek, Randburg 2125, South Africa.
Kaye PT; Department of Chemistry, Rhodes University, Grahamstown 6140, South Africa; Centre for Chemico- and Biomedicinal Research, Rhodes University, Grahamstown 6140, South Africa. Electronic address: P.Kaye@ru.ac.za.

Bioorg Chem ; 75: 310-316, 2017 12.

Article em En | MEDLINE | ID: mdl-29080495

Assuntos

Inibidores de Integrase de HIV/síntese química; Integrase de HIV/química; HIV-1/enzimologia; Quinolonas/química; Sobrevivência Celular/efeitos dos fármacos; Ativação Enzimática/efeitos dos fármacos; Células HEK293; Integrase de HIV/metabolismo; Inibidores de Integrase de HIV/metabolismo; Inibidores de Integrase de HIV/farmacologia; Transcriptase Reversa do HIV/antagonistas & inibidores; Transcriptase Reversa do HIV/metabolismo; Humanos; Quinolonas/metabolismo; Quinolonas/farmacologia; Relação Estrutura-Atividade

Palavras-chave

2-quinolones; Bioassay; HIV-1 integrase inhibitors; Morita_Baylis-Hillman; Synthesis

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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: HIV-1 / Quinolonas / Inibidores de Integrase de HIV / Integrase de HIV Limite: Humans Idioma: En Revista: Bioorg Chem Ano de publicação: 2017 Tipo de documento: Article País de afiliação: África do Sul

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