Author/Authors :
Ralph P. Robinson، نويسنده , , John A. Ragan، نويسنده , , Brian J. Cronin، نويسنده , , Kathleen M. Donahue، نويسنده , , Lori L. Lopresti-Morrow، نويسنده , , Peter G. Mitchell، نويسنده , , Lisa M. Reeves، نويسنده , , Sue A. Yocum، نويسنده ,
Abstract :
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 12IC50 = 0.15 μM).
