Synthesis and structure-activity relationship of 4-(2-aryl-cyclopropylamino)-quinoline-3-carbonitriles as EGFR tyrosine kinase inhibitors.

Pannala, Madhavi; Kher, Sunil; Wilson, Norma; Gaudette, John; Sircar, Ila; Zhang, Shao-Hui; Bakhirev, Alexei; Yang, Guang; Yuen, Phoebe; Gorcsan, Frank; Sakurai, Naoki; Barbosa, Miguel; Cheng, Jie-Fei

Pannala, Madhavi; Kher, Sunil; Wilson, Norma; Gaudette, John; Sircar, Ila; Zhang, Shao-Hui; Bakhirev, Alexei; Yang, Guang; Yuen, Phoebe; Gorcsan, Frank; Sakurai, Naoki; Barbosa, Miguel; Cheng, Jie-Fei.

Afiliação

Pannala M; Department of Chemistry, Tanabe Research Laboratories USA, Inc., 4540 Towne Centre Court, San Diego, CA 92121, USA.

Bioorg Med Chem Lett ; 17(21): 5978-82, 2007 Nov 01.

Article em En | MEDLINE | ID: mdl-17827009

ABSTRACT

ABSTRACT

Synthesis and structure-activity relationship of a series of 4-(2-aryl-cyclopropylamino)-quinoline-3-carbonitrile derivatives as EGFR inhibitors is described. Compounds 29 and 30 showed potent in vitro inhibitory activity in the enzymatic assay as well as in the functional cellular assay. They are moderately selective against other types of tyrosine kinases.

Assuntos

Inibidores Enzimáticos/química; Inibidores Enzimáticos/farmacologia; Receptores ErbB/antagonistas & inibidores; Nitrilas/química; Nitrilas/farmacologia; Quinolinas/química; Quinolinas/farmacologia; Inibidores Enzimáticos/síntese química; Nitrilas/síntese química; Quinolinas/síntese química; Relação Estrutura-Atividade

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Base de dados: MEDLINE Assunto principal: Quinolinas / Inibidores Enzimáticos / Receptores ErbB / Nitrilas Idioma: En Revista: Bioorg Med Chem Lett Assunto da revista: BIOQUIMICA / QUIMICA Ano de publicação: 2007 Tipo de documento: Article País de afiliação: Estados Unidos

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