Bioorganic and Medicinal Chemistry Letters p. 1719 - 1724 (1996)
Update date:2022-07-30
Topics:
Robinson, Ralph P.
Ragan, John A.
Cronin, Brian J.
Donahue, Kathleen M.
Lopresti-Morrow, Lori L.
Mitchell, Peter G.
Reeves, Lisa M.
Yocum, Sue A.
The effect of P1' Cα gem-disubstitution in a series of succinamide hydroxamate inhibitors of MMP-1 has been investigated. While in all cases P1' gem-disubstitution led to loss of potency relative to the corresponding P1' isobutyl and phenyl compounds 1 and 3, respectively, the loss of activity was less pronounced in certain instances, e.g., the P1' gem-cyclohexyl analogue 12 (IC50 = 0.15 μM).
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Doi:10.1016/S0968-0896(96)00266-0
(1997)Doi:10.1039/DT9960003411
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(1996)
