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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

  • Authors: Diana, P; Carbone, A; Barraja, P; Montalbano, A; Parrino, B; Lopergolo, A; Pennati, M; Zaffaroni, N; Cirrincione, G
  • Publication year: 2011
  • Type: Articolo in rivista (Articolo in rivista)
  • Key words: 3-(2-Phenyl-1,3-thiazol-4-yl)-1H-indoles; 3-(2-Phenyl-1,3-thiazol-4-yl)-1H-7-azaindoles; Nortopsentins; Antitumor activity
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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-7-azaindoles were obtained by Hantzsch reaction between substituted phenylthioamides and the a-bromoacetyl derivatives. Some azaindole derivatives, tested at the National Cancer Institute against a panel of ~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 IC50 values of 0.41 and 0.85 mm. These promising results will set the foundation for future investigations into the development of anticancer therapies.