2. Academic Validation
  3. Design and synthesis of N-phenylacetyl (sulfonyl) 4,5-dihydropyrazole derivatives as potential antitumor agents

Design and synthesis of N-phenylacetyl (sulfonyl) 4,5-dihydropyrazole derivatives as potential antitumor agents

  • Bioorg Med Chem Lett. 2011 May 15;21(10):2916-20. doi: 10.1016/j.bmcl.2011.03.066.
Xin-Hua Liu 1,  Ban-Feng Ruan,  Jing-Xin Liu,  Bao-An Song,  Ling-Hong Jing,  Jun Li,  Yang Yang,  Hai-Liang Zhu,  Xing-Bao Qi
Affiliations

Affiliation

  • 1 State Key Laboratory of Pharmaceutical Biotechnology, Nanjing University, Nanjing 210093, PR China.
PMID: 21486698 DOI: 10.1016/j.bmcl.2011.03.066
Abstract

A series of novel N-phenylacetyl (sulfonyl) 4,5-dihydropyrazole derivatives as potential Telomerase inhibitors were synthesized. The bioassay tests show that compound 4a exhibited high activity against human gastric Cancer cell SGC-7901, liver Cancer Hep-G2 and human prostate PC-3 cell lines with IC(50) values of 21.23±0.99, 29.43±0.32 and 30.89±1.07 μM, respectively. All title compounds were assayed for Telomerase inhibition by a modified TRAP assay, the results show that compound 4a can inhibit Telomerase with IC(50) value of 4.0±0.32 μM. Docking simulation was performed to position compound 4a into the Telomerase (3DU6) active site to determine the probable binding model.

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