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Discovery and optimization of novel benzothiophene-3-carboxamides as highly potent inhibitors of Aurora kinases A and B.
Gyulavári, Pál; Szokol, Bálint; Szabadkai, István; Brauswetter, Diána; Bánhegyi, Péter; Varga, Attila; Markó, Péter; Boros, Sándor; Illyés, Eszter; Szántai-Kis, Csaba; Krekó, Marcell; Czudor, Zsófia; Orfi, László.
Afiliação
  • Gyulavári P; MTA-SE Pathobiochemistry Research Group, 37-43. Tuzoltó u., Budapest 1094, Hungary.
  • Szokol B; Vichem Chemie Research Ltd., 15. Herman Ottó u., Budapest 1022, Hungary.
  • Szabadkai I; Vichem Chemie Research Ltd., 15. Herman Ottó u., Budapest 1022, Hungary.
  • Brauswetter D; MTA-SE Pathobiochemistry Research Group, 37-43. Tuzoltó u., Budapest 1094, Hungary.
  • Bánhegyi P; Vichem Chemie Research Ltd., 15. Herman Ottó u., Budapest 1022, Hungary.
  • Varga A; MTA-SE Pathobiochemistry Research Group, 37-43. Tuzoltó u., Budapest 1094, Hungary.
  • Markó P; Vichem Chemie Research Ltd., 15. Herman Ottó u., Budapest 1022, Hungary.
  • Boros S; Vichem Chemie Research Ltd., 15. Herman Ottó u., Budapest 1022, Hungary.
  • Illyés E; Vichem Chemie Research Ltd., 15. Herman Ottó u., Budapest 1022, Hungary.
  • Szántai-Kis C; Vichem Chemie Research Ltd., 15. Herman Ottó u., Budapest 1022, Hungary.
  • Krekó M; Department of Pharmaceutical Chemistry, Semmelweis University, 9. Hogyes Endre u., Budapest 1092, Hungary.
  • Czudor Z; Department of Pharmaceutical Chemistry, Semmelweis University, 9. Hogyes Endre u., Budapest 1092, Hungary.
  • Orfi L; Vichem Chemie Research Ltd., 15. Herman Ottó u., Budapest 1022, Hungary; Department of Pharmaceutical Chemistry, Semmelweis University, 9. Hogyes Endre u., Budapest 1092, Hungary. Electronic address: orfi.laszlo@pharma.semmelweis-univ.hu.
Bioorg Med Chem Lett ; 28(19): 3265-3270, 2018 10 15.
Article em En | MEDLINE | ID: mdl-30143423
ABSTRACT
Aurora kinases as regulators of cell division have become promising therapeutic targets recently. Here we report novel, low molecular weight benzothiophene-3-carboxamide derivatives designed and optimized for inhibiting Aurora kinases. The most effective compound 36 inhibits Aurora kinases in vitro in the nanomolar range and diminishes HCT 116 cell viability blocking cytokinesis and inducing apoptosis. According to western blot analysis, the lead molecule inhibits Aurora kinases equipotently to VX-680 (Tozasertib) and similarly synergizes with other targeted drugs.
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Tiofenos / Inibidores de Proteínas Quinases / Aurora Quinase A / Aurora Quinase B / Amidas Limite: Humans Idioma: En Revista: Bioorg Med Chem Lett Assunto da revista: BIOQUIMICA / QUIMICA Ano de publicação: 2018 Tipo de documento: Article País de afiliação: Hungria
Texto completo
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Tiofenos / Inibidores de Proteínas Quinases / Aurora Quinase A / Aurora Quinase B / Amidas Limite: Humans Idioma: En Revista: Bioorg Med Chem Lett Assunto da revista: BIOQUIMICA / QUIMICA Ano de publicação: 2018 Tipo de documento: Article País de afiliação: Hungria