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Novel compounds with potent CDK9 inhibitory activity for the treatment of myeloma.
Czudor, Zsófia; Balogh, Mária; Bánhegyi, Péter; Boros, Sándor; Breza, Nóra; Dobos, Judit; Fábián, Márk; Horváth, Zoltán; Illyés, Eszter; Markó, Péter; Sipos, Anna; Szántai-Kis, Csaba; Szokol, Bálint; Orfi, László.
Afiliação
  • Czudor Z; Department of Pharmaceutical Chemistry, Semmelweis University, Hogyes Endre u. 9, 1092 Budapest, Hungary.
  • Balogh M; Vichem Chemie Research Ltd., Herman Ottó u. 15., 1022 Budapest, Hungary.
  • Bánhegyi P; Vichem Chemie Research Ltd., Herman Ottó u. 15., 1022 Budapest, Hungary.
  • Boros S; Vichem Chemie Research Ltd., Herman Ottó u. 15., 1022 Budapest, Hungary.
  • Breza N; Vichem Chemie Research Ltd., Herman Ottó u. 15., 1022 Budapest, Hungary.
  • Dobos J; Vichem Chemie Research Ltd., Herman Ottó u. 15., 1022 Budapest, Hungary.
  • Fábián M; Department of Pharmaceutical Chemistry, Semmelweis University, Hogyes Endre u. 9, 1092 Budapest, Hungary.
  • Horváth Z; Vichem Chemie Research Ltd., Herman Ottó u. 15., 1022 Budapest, Hungary.
  • Illyés E; Vichem Chemie Research Ltd., Herman Ottó u. 15., 1022 Budapest, Hungary.
  • Markó P; Vichem Chemie Research Ltd., Herman Ottó u. 15., 1022 Budapest, Hungary.
  • Sipos A; Vichem Chemie Research Ltd., Herman Ottó u. 15., 1022 Budapest, Hungary.
  • Szántai-Kis C; Vichem Chemie Research Ltd., Herman Ottó u. 15., 1022 Budapest, Hungary.
  • Szokol B; Vichem Chemie Research Ltd., Herman Ottó u. 15., 1022 Budapest, Hungary.
  • Orfi L; Department of Pharmaceutical Chemistry, Semmelweis University, Hogyes Endre u. 9, 1092 Budapest, Hungary; Vichem Chemie Research Ltd., Herman Ottó u. 15., 1022 Budapest, Hungary. Electronic address: orfi.laszlo@pharma.semmelweis-univ.hu.
Bioorg Med Chem Lett ; 28(4): 769-773, 2018 02 15.
Article em En | MEDLINE | ID: mdl-29329658
ABSTRACT
Cyclin-dependent kinases (CDKs) and Polo-like kinases (PLKs) play key role in the regulation of the cell cycle. The aim of our study was originally the further development of our recently discovered polo-like kinase 1 (PLK1) inhibitors. A series of new 2,4-disubstituted pyrimidine derivatives were synthesized around the original hit, but their PLK1 inhibitory activity was very poor. However the novel compounds showed nanomolar CDK9 inhibitory activity and very good antiproliferative effect on multiple myeloma cell lines (RPMI-8226).
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Pirimidinas / Quinase 9 Dependente de Ciclina / Inibidores de Proteínas Quinases / Mieloma Múltiplo / Antineoplásicos 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
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Pirimidinas / Quinase 9 Dependente de Ciclina / Inibidores de Proteínas Quinases / Mieloma Múltiplo / Antineoplásicos 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