New substituted 4-arylaminoquinazolines as potent inhibitors of breast tumor cell lines: In vitro and docking experiments

Autor(es)

de Oliveira, Andre N. ^[1] ; Bocca, Cleverson C. ^[2] ; Carvalho, Joao E. ^[3] ; Ruiz, Ana Lucia G. ^[3] ; Silva, Thiago P. ^[2] ; Rittner, Roberto ^[2] ; Hoehr, Nelci F. ^[1]

Afiliação do(s) autor(es)

^[1] Univ Estadual Campinas, Sch Med Sci, Dept Clin Pathol, BR-13083887 Campinas, SP - Brazil

^[2] Univ Estadual Campinas, Phys Organ Chem Lab, Inst Chem, BR-13083970 Campinas, SP - Brazil

^[3] Univ Estadual Campinas, Pluridisciplinary Ctr Chem Biol & Agr Res, BR-13084971 Campinas, SP - Brazil

• Tipo de documento: Artigo Científico
• Fonte: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY; v. 45, n. 9, p. 4339-4342, SEP 2010.
• Citações Web of Science: 10

Resumo

The arylquinazolines represent significant advances in the clinical management of breast cancer. Nevertheless some confirmatory studies must be considered to foster the use of anti-EGFR therapies including safety and clinical use. Two 4-arylaminoquinazoline derivatives, recently synthesized, were tested as kinase inhibitors and their citotoxicities showed potent growth inhibitory activity in breast tumor cell lines (MCF-7). The predicted complex structure of quinazoline inhibitors with EGFR protein from molecular docking provided a stereoview of the binding site correlated with structure activity, affording important information about structure-based drug design. (C) 2010 Published by Elsevier Masson SAS. (AU)

• Processo FAPESP: 05/59649-0 - Estudos de estrutura eletrônica e molecular através de métodos espectroscópicos e cálculos teóricos
• Beneficiário: Roberto Rittner Neto
• Modalidade de apoio: Auxílio à Pesquisa - Temático