Screening, synthesis, crystal structure, and molecular basis of 6-amino-4-phenyl-1,4-dihydropyrano[2,3-c]pyrazole-5-carbonitriles as novel AKR1C3 inhibitors.

Zheng, Xuehua; Jiang, Zan; Li, Xiaolin; Zhang, Chen; Li, Zhe; Wu, Yinuo; Wang, Xinhua; Zhang, Chao; Luo, Hai-Bin; Xu, Jun; Wu, Deyan

Zheng, Xuehua; Jiang, Zan; Li, Xiaolin; Zhang, Chen; Li, Zhe; Wu, Yinuo; Wang, Xinhua; Zhang, Chao; Luo, Hai-Bin; Xu, Jun; Wu, Deyan.

Afiliação

Zheng X; Key Laboratory of Molecular Target & Clinical Pharmacology, School of Pharmaceutical Sciences & the Fifth Affiliated Hospital, Guangzhou Medical University, Guangzhou 511436, China.
Jiang Z; Key Laboratory of Molecular Target & Clinical Pharmacology, School of Pharmaceutical Sciences & the Fifth Affiliated Hospital, Guangzhou Medical University, Guangzhou 511436, China.
Li X; School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, China.
Zhang C; School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, China.
Li Z; School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, China.
Wu Y; School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, China.
Wang X; Key Laboratory of Molecular Target & Clinical Pharmacology, School of Pharmaceutical Sciences & the Fifth Affiliated Hospital, Guangzhou Medical University, Guangzhou 511436, China.
Zhang C; Key Laboratory of Molecular Target & Clinical Pharmacology, School of Pharmaceutical Sciences & the Fifth Affiliated Hospital, Guangzhou Medical University, Guangzhou 511436, China.
Luo HB; School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, China.
Xu J; School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, China. Electronic address: junxu@biochemomes.com.
Wu D; School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, China. Electronic address: wudeyan3@mail.sysu.edu.cn.

Bioorg Med Chem ; 26(22): 5934-5943, 2018 12 01.

Article em En | MEDLINE | ID: mdl-30429100

Assuntos

Membro C3 da Família 1 de alfa-Ceto Redutase/antagonistas & inibidores; Inibidores Enzimáticos/farmacologia; Nitrilas/farmacologia; Membro C3 da Família 1 de alfa-Ceto Redutase/metabolismo; Cristalografia por Raios X; Relação Dose-Resposta a Droga; Avaliação Pré-Clínica de Medicamentos; Inibidores Enzimáticos/síntese química; Inibidores Enzimáticos/química; Humanos; Modelos Moleculares; Estrutura Molecular; Nitrilas/síntese química; Nitrilas/química; Proteínas Recombinantes/metabolismo; Relação Estrutura-Atividade

Palavras-chave

1,4-Dihydropyrano[2,3-c]pyrazole; AKR1C3 inhibitors; Castration-resistant prostate cancer; Crystal structure; Synthesis

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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Inibidores Enzimáticos / Membro C3 da Família 1 de alfa-Ceto Redutase / Nitrilas Tipo de estudo: Diagnostic_studies / Screening_studies Limite: Humans Idioma: En Revista: Bioorg Med Chem Assunto da revista: BIOQUIMICA / QUIMICA Ano de publicação: 2018 Tipo de documento: Article País de afiliação: China País de publicação: Reino Unido

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