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

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Given the potent antimicrobial, antiviral, and antitumor activities of many natural products, there is an increasing interest inthe 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 substitutedphenylthioamides and the a-bromoacetyl derivatives. Some azaindole derivatives, tested at the National Cancer Instituteagainst a panel of ~60 tumor cell lines derived from nine human cancer cell types, showed inhibitory effects against allcell lines investigated at micromolar to nanomolar concentrations. Two of them exhibited a high affinity for CDK1, with IC50values of 0.41 and 0.85 mm. These promising results will set the foundation for future investigations into the development of anticancer therapies.
Lingua originaleEnglish
pagine (da-a)1300-1309
Numero di pagine10
Stato di pubblicazionePublished - 2011

All Science Journal Classification (ASJC) codes

  • Biochemistry
  • Molecular Medicine
  • Pharmacology
  • Drug Discovery
  • ???subjectarea.asjc.3000.3000???
  • Organic Chemistry

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