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Synthesis and Antitumor Activity studies of some new Fused 1,2,4-triazole Derivatives carrying 2,4-dichloro-5-fluorophenyl moiety

Bhat, Subrahmanya K and Poojary, Boja and Prasad, Jagadeesh D and Naik, Prashantha and Holla, Shivarama B (2009) Synthesis and Antitumor Activity studies of some new Fused 1,2,4-triazole Derivatives carrying 2,4-dichloro-5-fluorophenyl moiety. European Journal of Medicinal Chemistry, 44 (12). pp. 5066-5070. ISSN 0223-5234

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Abstract

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 mM

Item Type: Article
Uncontrolled Keywords: 1,2,4-Triazoles 1,3,4-thiadiazines 2,4-dichloro-5- fuorophenyl Anticancer activity GI50 values
Subjects: Engineering > MIT Manipal > Chemistry
Depositing User: MIT Library
Date Deposited: 22 Jul 2011 11:03
Last Modified: 22 Jul 2011 11:03
URI: http://eprints.manipal.edu/id/eprint/894

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