Drug Discoveries & Therapeutics
Online ISSN : 1881-784X
Print ISSN : 1881-7831
ISSN-L : 1881-7831
Original Articles
Sulfonyl phosphonic 1,4-dithia-7-azaspiro[4,4]nonane derivatives as matrix metalloproteinase inhibitors: Synthesis, a docking study, and biological evaluation
Hao ZhangXuan LiXuejian WangWenfang XuJian Zhang
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2017 Volume 11 Issue 3 Pages 118-125


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.

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© 2017 International Research and Cooperation Association for Bio & Socio-Sciences Advancement
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