The synthesis and biological evaluation of non-peptidic matrix metalloproteinase inhibitors.
Article Details
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Martin FM, Beckett RP, Bellamy CL, Courtney PF, Davies SJ, Drummond AH, Dodd R, Pratt LM, Patel SR, Ricketts ML, Todd RS, Tuffnell AR, Ward JW, Whittaker M
The synthesis and biological evaluation of non-peptidic matrix metalloproteinase inhibitors.
Bioorg Med Chem Lett. 1999 Oct 4;9(19):2887-92.
- PubMed ID
- 10522712 [ View in PubMed]
- Abstract
Novel sulfonamide matrix metalloproteinase inhibitors of general formula (9) were synthesised by a route involving a stereoselective conjugate addition reaction. Enzyme selectivity was found to be dependant on the nature of the sulfonamide substituents. Compounds (9f, 9q) are potent selective collagenase inhibitors with good oral bioavailability.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Marimastat 72 kDa type IV collagenase IC 50 (nM) 6 N/A N/A Details Marimastat Collagenase 3 IC 50 (nM) 2 N/A N/A Details Marimastat Interstitial collagenase IC 50 (nM) 5 N/A N/A Details Marimastat Neutrophil collagenase IC 50 (nM) 2 N/A N/A Details Marimastat Stromelysin-1 IC 50 (nM) 200 N/A N/A Details