Sulphonamide 1,4-dithia-7-azaspiro[4,4]nonane derivatives as gelatinase A inhibitors. Academic Article uri icon


  • Gelatinase A, a zinc-containing endopeptidase, has been shown to be an essential therapeutic target for tumor intervention owing to its participation in almost all types of solid tumors. Based on our previous work with respect to quinoxalinone peptidomimetics, a novel series of sulphonamide-containing 1,4-dithia-7-azaspiro[4,4]nonane (DAN) derivatives have been synthesized and evaluated as potential gelatinase A inhibitors hereby. The results revealed that the majority of tested compounds displayed satisfactory inhibition activity against gelatinase A. Among the tested compounds, 2b, 3a, 4a-d, 6a, 6d, 7a-d exhibited more potent gelatinase A inhibition than the positive control LY52. Furthermore, two test compounds 2b and 6a demonstrated moderate anti-proliferative in vitro and anti-metastatic activities in vivo, which might be utilized as potential leads in future chemical optimization.

published proceedings

  • Bioorg Med Chem

altmetric score

  • 0.25

author list (cited authors)

  • Shi, L., Wang, Q., Wang, H., Zhou, H., Li, Y., & Li, X.

citation count

  • 8

complete list of authors

  • Shi, Leilei||Wang, Qiang||Wang, Haina||Zhou, Hua||Li, Yonggang||Li, Xun

publication date

  • December 2013