Bhupender Singh 23 articles
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Synthesis of 3-Phenylpyrazolopyrimidine-1,2,3-Triazole Conjugates and Evaluation of their Src Kinase Inhibitory and Anticancer Activities

  • Posted by Bhupender Singh
  • January 31, 2011 9:05:04 AM TLT
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A series of two classes of 3-phenylpyrazolopyrimidine-1,2,3-triazole conjugates were synthesized using click chemistry approach. All compounds were evaluated for inhibition of Src kinase and human ovarian adenocarcinoma (SK-Ov-3), breast carcinoma (MDA-MB-361), and colon adenocarcinoma (HT-29). Hexyl triazolyl-substituted 3-phenylpyrazolopyrimidine exhibited inhibition of Src kinase with an IC50 value of 5.6 μM. 4-Methoxyphenyl triazolyl-substituted 3-phenylpyrazolopyrimidine inhibited the cell proliferation of HT-29 and SK-Ov-3 by 73% and 58%, respectively, at a concentration of 50 μM.

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  • Authors Anil Kumar, Israr Ahmad, Bhupender S. Chhikara, Rakesh Tiwari, Deendayal Mandal and Keykavous Parang
  • Affiliation Department of Chemistry, Birla Institute of Technology and Science, Pilani-333031, Rajasthan, India Department of Biomedical and Pharmaceutical Sciences, University of Rhode Island, Kingston, RI, 02881 USA
  • Journal name Bioorganic and Medicinal Chemistry Letters
  • Year 2011
  • Volume, Issue 21, 5
  • Page Number 1342-1346
  • DOI No. 10.1016/j.bmcl.2011.01.047
  • Link http://dx.doi.org/10.1016/j.bmcl.2011.01.047
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