Synthesis and antitumor activity studies of some new fused 1,2,4-triazole derivatives carrying 2,4-dichloro-5-fluorophenyl moiety

K. Subrahmanya Bhat, Boja Poojary, D. Jagadeesh Prasad, Prashantha Naik, B. Shivarama Holla

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A series of 3-(2,4-dichloro-5-fluorophenyl)-6-(substituted phenyl)-1,2,4-triazolo[3,4-b]-1,3,4-thiadiazines (4) (Fig. 1) have been synthesized by the cyclization of 3-(2,4-dichloro-5-fluorophenyl)-1,2,4-triazol-5-thiol (3) with substituted phenacyl bromides. All the newly synthesized compounds were confirmed by IR, 1H NMR and mass spectral studies. Among the compounds tested for their antitumor activity three compounds exhibited in vitro antitumor activity with moderate to excellent growth inhibition against a panel of sixty cancer cell lines of leukemia, non-small cell lung cancer, melanoma, ovarian cancer, prostate and breast cancer. The compound 4d showed promising antiproliferative activity with GI50 values in the range of 1.06-25.4 μM.

Original languageEnglish
Pages (from-to)5066-5070
Number of pages5
JournalEuropean Journal of Medicinal Chemistry
Issue number12
Publication statusPublished - 12-2009


All Science Journal Classification (ASJC) codes

  • Drug Discovery
  • Organic Chemistry
  • Pharmacology

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