2. Academic Validation
  3. Design and synthesis of novel 2-methyl-4,5-substitutedbenzo[f]-3,3a,4,5-tetrahydro-pyrazolo[1,5-d][1,4]oxazepin-8(7H)-one derivatives as telomerase inhibitors

Design and synthesis of novel 2-methyl-4,5-substitutedbenzo[f]-3,3a,4,5-tetrahydro-pyrazolo[1,5-d][1,4]oxazepin-8(7H)-one derivatives as telomerase inhibitors

  • Bioorg Med Chem Lett. 2013 Feb 1;23(3):720-3. doi: 10.1016/j.bmcl.2012.11.101.
Xin-Hua Liu 1,  Ying-Ming Jia,  Bao-An Song,  Zhi-xiang Pang,  Song Yang
Affiliations

Affiliation

  • 1 Key Laboratory of Green Pesticide and Agriculture Bioengineering, Ministry of Education, Guizhou University, Guiyang 550025, PR China. xhliuhx@163.com
PMID: 23265905 DOI: 10.1016/j.bmcl.2012.11.101
Abstract

Eight novel 4,5-tetrahydropyrazolo[1,5-d][1,4]oxazepine derivatives have been synthesized and purified to be screened for Anticancer activity. By a modified TRAP assay, some titled compounds were tested against Telomerase, and compound 4a showed the most potent inhibitory activity with IC(50) value at 0.78 ± 0.22 μM. Western blot assays showed that compounds 4a and 4b could inhibit expression of Cyclin D1, TERT, phospho-AKT and PI3K/Akt pathway.

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