4.5 Article

Synthesis and Antitumor Activity of 3-(2-Phenyl-1,3-thiazol-4-yl)-1H-indoles and 3-(2-Phenyl-1,3-thiazol-4-yl)-1H-7-azaindoles

Journal

CHEMMEDCHEM
Volume 6, Issue 7, Pages 1300-1309

Publisher

WILEY-BLACKWELL
DOI: 10.1002/cmdc.201100078

Keywords

azaindoles; antitumor agents; indoles; kinases; nortopsentins

Funding

  1. Ministero dell'Istruzione dell'Universita e della Ricerca
  2. Associazione Italiana per la Ricerca sul Cancro

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Given the potent antimicrobial, antiviral, and antitumor activities of many natural products, there is an increasing interest in the synthesis of new molecules based on natural compound scaffolds. Based on a 2,4-bis(3'-indolyl) imidazole skeleton, two new series of phenylthiazolylindoles and phenylthiazolyl-7azaindoles were obtained by Hantzsch reaction between substituted phenylthioamides and the alpha-bromoacetyl derivatives. Some azaindole derivatives, tested at the National Cancer Institute against a panel of similar to 60 tumor cell lines derived from nine human cancer cell types, showed inhibitory effects against all cell lines investigated at micromolar to nanomolar concentrations. Two of them exhibited a high affinity for CDK1, with IC(50) values of 0.41 and 0.85 mu m. These promising results will set the foundation for future investigations into the development of anticancer therapies.

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