Bioorganic and Medicinal Chemistry Letters p. 127 - 132 (1999)
Update date:2022-08-05
Topics:
Reiter, Lawrence A.
Rizzi, James P.
Pandit, Jayvardan
Lasut, Michael J.
McGahee, Shunda M.
Parikh, Vinod D.
Blake, James F.
Danley, Dennis E.
Laird, Ellen R.
Lopez-Anaya, Arturo
Lopresti-Morrow, Lori L.
Mansour, Mahmoud N.
Martinelli, Gary J.
Mitchell, Peter G.
Owens, Brian S.
Pauly, Thomas A.
Reeves, Lisa M.
Schulte, Gayle K.
Yocum, Sue A.
Through the use of empirical and computational methods, phosphinate- based inhibitors of MMP-1 and MMP-13 that bind into the S2 pocket of these enzymes were designed. The synthesis and testing of 2 suggested that binding was occuring as hypothesized. Structure determination of a co-crystal of 2 bound to the catalytic domain of MMP-1 confirmed the binding mode. Substituents binding into S2, S1', S2' and S3', were optimized yielding compounds with low double-digit nM IC50's against these enzymes.
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