Discovery of the 3-Amino-1,2,4-triazine-Based Library as Selective PDK1 Inhibitors with Therapeutic Potential in Highly Aggressive Pancreatic Ductal Adenocarcinoma.

Carbone, Daniela; De Franco, Michele; Pecoraro, Camilla; Bassani, Davide; Pavan, Matteo; Cascioferro, Stella; Parrino, Barbara; Cirrincione, Girolamo; Dall'Acqua, Stefano; Moro, Stefano; Gandin, Valentina; Diana, Patrizia

Carbone, Daniela; De Franco, Michele; Pecoraro, Camilla; Bassani, Davide; Pavan, Matteo; Cascioferro, Stella; Parrino, Barbara; Cirrincione, Girolamo; Dall'Acqua, Stefano; Moro, Stefano; Gandin, Valentina; Diana, Patrizia.

Afiliação

Carbone D; Department of Biological, Chemical, and Pharmaceutical Sciences and Technologies (STEBICEF), University of Palermo, Via Archirafi 32, 90123 Palermo, Italy.
De Franco M; Department of Pharmaceutical and Pharmacological Sciences, University of Padova, Via F. Marzolo 5, 35131 Padova, Italy.
Pecoraro C; Department of Biological, Chemical, and Pharmaceutical Sciences and Technologies (STEBICEF), University of Palermo, Via Archirafi 32, 90123 Palermo, Italy.
Bassani D; Molecular Modeling Section (MMS), Department of Pharmaceutical and Pharmacological Sciences, University of Padova, Via F. Marzolo 5, 35131 Padova, Italy.
Pavan M; Molecular Modeling Section (MMS), Department of Pharmaceutical and Pharmacological Sciences, University of Padova, Via F. Marzolo 5, 35131 Padova, Italy.
Cascioferro S; Department of Biological, Chemical, and Pharmaceutical Sciences and Technologies (STEBICEF), University of Palermo, Via Archirafi 32, 90123 Palermo, Italy.
Parrino B; Department of Biological, Chemical, and Pharmaceutical Sciences and Technologies (STEBICEF), University of Palermo, Via Archirafi 32, 90123 Palermo, Italy.
Cirrincione G; Department of Biological, Chemical, and Pharmaceutical Sciences and Technologies (STEBICEF), University of Palermo, Via Archirafi 32, 90123 Palermo, Italy.
Dall'Acqua S; Department of Pharmaceutical and Pharmacological Sciences, University of Padova, Via F. Marzolo 5, 35131 Padova, Italy.
Moro S; Molecular Modeling Section (MMS), Department of Pharmaceutical and Pharmacological Sciences, University of Padova, Via F. Marzolo 5, 35131 Padova, Italy.
Gandin V; Department of Pharmaceutical and Pharmacological Sciences, University of Padova, Via F. Marzolo 5, 35131 Padova, Italy.
Diana P; Department of Biological, Chemical, and Pharmaceutical Sciences and Technologies (STEBICEF), University of Palermo, Via Archirafi 32, 90123 Palermo, Italy.

Int J Mol Sci ; 24(4)2023 Feb 12.

Article em En | MEDLINE | ID: mdl-36835086

Assuntos

Adenocarcinoma; Neoplasias Pancreáticas; Piruvato Desidrogenase Quinase de Transferência de Acetil; Bibliotecas de Moléculas Pequenas; Humanos; Adenocarcinoma/tratamento farmacológico; Adenocarcinoma/metabolismo; Neoplasias Pancreáticas/tratamento farmacológico; Neoplasias Pancreáticas/metabolismo; Proteínas Serina-Treonina Quinases/antagonistas & inibidores; Proteínas Serina-Treonina Quinases/metabolismo; Proteínas Proto-Oncogênicas p21(ras)/efeitos dos fármacos; Proteínas Proto-Oncogênicas p21(ras)/metabolismo; Piruvato Desidrogenase Quinase de Transferência de Acetil/antagonistas & inibidores; Bibliotecas de Moléculas Pequenas/química; Bibliotecas de Moléculas Pequenas/farmacologia; Inibidores de Proteínas Quinases/química; Inibidores de Proteínas Quinases/uso terapêutico; Neoplasias Pancreáticas

Palavras-chave

3-amino-1,2,4-triazine derivatives; Kras-mutated pancreatic ductal adenocarcinoma; PDK inhibitors; antitumor agents; bis-indole derivatives; ligand-based homology modeling

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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Neoplasias Pancreáticas / Adenocarcinoma / Bibliotecas de Moléculas Pequenas / Piruvato Desidrogenase Quinase de Transferência de Acetil Limite: Humans Idioma: En Revista: Int J Mol Sci Ano de publicação: 2023 Tipo de documento: Article País de afiliação: Itália

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