Related Experiment Video
Updated: Feb 25, 2026
Constructing Thioether/Vinyl Sulfide-tethered Helical Peptides Via Photo-induced Thiol-ene/yne Hydrothiolation
Published on: August 1, 2018
Sulfonyl phosphonic 1,4-dithia-7-azaspiro[4,4]nonane derivatives as matrix metalloproteinase inhibitors: Synthesis, a
Hao Zhang1, Xuan Li2, Xuejian Wang1
1Department of Medical Chemistry, School of Pharmacy, Weifang Medical University.
Abstract:
A series of novel sulfonyl phosphonic 1,4-dithia-7-azaspiro[4,4]nonane derivatives were designed, synthesized, and assayed for their activity against matrix metalloproteinase-2 (MMP-2). Results indicated that all of the compounds exhibited moderate inhibitory activity against MMP-2 compared to LY52 (the control) (IC50 = 0.95 ± 0.09 µM). Several selected compounds were also examined for their antiproliferative activity against SKOV3, HL60, and A549 cells. Notably, all of the tested compounds had slightly lower antiproliferative activity against SKOV3 cells than that of LY52. Compound 6d displayed the greatest inhibitory activity in an enzymatic assay and a cell-based assay, which means that this compound is a good candidate for further development of phosphonate-based MMP inhibitors.
