Synthesis and antiproliferative activity of substituted 3[2-(1H-indol-3-yl)-1,3-thiazol-4-yl]-1H-pyrrolo[3,2-b]pyridines, marine alkaloid nortopsentin analogues

Alessandra Montalbano, Virginia Spano', Barbara Parrino, Anna Carbone, Girolamo Cirrincione, Paola Barraja, Patrizia Diana, Alessia Lopergolo, Sbarra, Virginia Spanò, Barbara Parrino, Doldi, Anna Carbone, Marzia Pennati, Alessandra Montalbano, Paola Barraja, Girolamo Cirrincione, Patrizia Diana, Nadia Zaffaroni

Research output: Contribution to journalArticlepeer-review

44 Citations (Scopus)

Abstract

A large number of indolyl-4-azaindolyl thiazoles, nortopsentin analogues, were conveniently synthesized. The antiproliferative activity of the new derivatives was examined against four human tumor cell lines with different histologic origin. Seven derivatives consistently reduced the growth of the experimental models independently of TP53 gene status and exhibited the highest activity against the malignant peritoneal mesothelioma (STO) cell line. The most active compound of this series acts as a CDK1 inhibitor, and was found to cause cell cycle arrest at G2/M phase, to induce apoptosis by preventing the phosphorylation of survivin in Thr34 and to increase the cytotoxic activity of paclitaxel in STO cells.
Original languageEnglish
Pages (from-to)1654-1666
Number of pages13
JournalCurrent Medicinal Chemistry
Volume21
Publication statusPublished - 2014

All Science Journal Classification (ASJC) codes

  • General Medicine
  • Biochemistry
  • Molecular Medicine
  • Pharmacology
  • Drug Discovery
  • Organic Chemistry

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