Novel pyrazolopyrimidine derivatives as tyrosine kinase inhibitors with antitumoral activity in vitro and in vivo in papillary dedifferentiated thyroid cancer

Alessandro Antonelli, Guido Bocci, Concettina La Motta, Silvia Martina Ferrari, Poupak Fallahi, Anna Fioravanti, Stefania Sartini, Michele Minuto, Simona Piaggi, Alessandro Corti, Greta Alì, Piero Berti, Gabriella Fontanini, Romano Danesi, Federico Da Settimo, Paolo Miccoli

Research output: Contribution to journalArticlepeer-review

Abstract

Aim: We have studied the antitumoral activity of two new pyrazolo[3,4-d]pyrimidine compounds (CLM3 and CLM29) in primary papillary dedifferentiated thyroid cancer (DePTC) cells. Methods: The antiproliferative effect was tested in DePTC cells obtained at reoperation from patients with recurrence of the tumor. The concentrations of CLM3 and CLM29 used in the in vitro experiments were 1, 10, 30, and 50 μM. Results: Proliferation assays in DePTC cells showed a significant reduction of proliferation by CLM3 and CLM29, which was by 12% with CLM3 (the most potent compound) 10 μM, 43% with CLM3 30 μM, and 60% with CLM3 50 μM. CLM3 and CLM29 increased the percentage of apoptotic cells in DePTC cells dose dependently (P

Original languageEnglish
JournalJournal of Clinical Endocrinology and Metabolism
Volume96
Issue number2
DOIs
Publication statusPublished - Feb 2011

ASJC Scopus subject areas

  • Biochemistry
  • Clinical Biochemistry
  • Endocrinology
  • Biochemistry, medical
  • Endocrinology, Diabetes and Metabolism

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