2. Academic Validation
  3. Synthesis and cytotoxicity of 3,4-disubstituted-5-(3,4,5-trimethoxyphenyl)-4H-1,2,4-triazoles and novel 5,6-dihydro-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazole derivatives bearing 3,4,5-trimethoxyphenyl moiety

Synthesis and cytotoxicity of 3,4-disubstituted-5-(3,4,5-trimethoxyphenyl)-4H-1,2,4-triazoles and novel 5,6-dihydro-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazole derivatives bearing 3,4,5-trimethoxyphenyl moiety

  • Bioorg Med Chem Lett. 2012 Jul 1;22(13):4471-4. doi: 10.1016/j.bmcl.2012.03.023.
Pei-Liang Zhao 1,  An-Na Duan,  Min Zou,  Hai-Kui Yang,  Wen-Wei You,  Shu-Guang Wu
Affiliations

Affiliation

  • 1 Department of Chemistry, College of Pharmaceutical Sciences, Southern Medical University, Guangzhou 510515, PR China.
PMID: 22647723 DOI: 10.1016/j.bmcl.2012.03.023
Abstract

A series of 3,4-disubstituted-5-(3,4,5-trimethoxyphenyl)-4H-1,2,4-triazoles and some novel 5,6-dihydro-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazoles bearing 3,4,5-trimethoxyphenyl moiety were synthesized and screened for their Anticancer activity. The preliminary bioassay results indicated that compounds 14 and 16 showed much stronger cytotoxicity than Doxorubicin against HepG2 cell lines with IC(50) values of 0.58 and 3.17 μM, respectively. Meanwhile compound 16 also exhibited a broad spectrum of antitumor activity against MCF-7 and MKN45 with IC(50) values of 10.92 and 13.79 μM, respectively.

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