α-Sulfone-α-piperidine and α-tetrahydropyranyl hydroxamates were explored that are potent inhibitors of MMP’s-2, -9, and -13 that spare MMP-1, with oral efficacy in inhibiting tumor growth in mice and left-ventricular hypertrophy in rats and in the bovine cartilage degradation ex vivo explant system. α-Piperidine 19v (SC-78080/SD-2590) was selected for development toward the initial indication of cancer, while α-piperidine and α-tetrahydropyranyl hydroxamates 19w (SC-77964) and 9i (SC-77774), respectively, were identified as backup compounds
We recently reported the discovery of AM-8553 (<b>1</b>), a potent and selective piperidinone inhibi...
Osteoarthritis (OA) is the leading cause of joint pain and disability in middle-aged and elderly pat...
Matrix metalloproteinases (MMPs) are a family of enzymes involved at different stages of cancer prog...
α-Sulfone-α-piperidine and α-tetrahydropyranyl hydroxamates were explored that are potent inhibitors...
A series of phenyl piperidine α-sulfone hydroxamate derivatives has been prepared utilizing a combin...
A series of N-aryl isonipecotamide α-sulfone hydroxamate derivatives has been prepared utilizing a c...
A series of α-alkyl-α-amino-β-sulphone hydroxamates was prepared and evaluated for potency versus MM...
α-Piperidine-β-sulfone hydroxamate derivatives were explored that are potent for matrix metalloprote...
A series of α-amino-β-sulphone hydroxamates was prepared and evaluated for potency versus MMP-13 and...
Purpose: The implication of matrix metalloproteinases (MMPs) in the major stages of cancer progressi...
Matrix metalloproteinase 7 (MMP-7) is a member of the MMP superfamily and is able to degrade extrace...
Continuing our interest in designing compounds preferentially potent and selective for MMP-13, we re...
Collagen degradation and proMMP-2 activation are major functions of MT1-MMP to promote cancer cell i...
Gelatinase B or matrix metalloproteinase-9 (MMP-9) (EC 3.4.24.35) is increased in inflammatory proce...
Seeking compounds preferentially potent and selective for MMP-13, we reported in the preceding Lette...
We recently reported the discovery of AM-8553 (<b>1</b>), a potent and selective piperidinone inhibi...
Osteoarthritis (OA) is the leading cause of joint pain and disability in middle-aged and elderly pat...
Matrix metalloproteinases (MMPs) are a family of enzymes involved at different stages of cancer prog...
α-Sulfone-α-piperidine and α-tetrahydropyranyl hydroxamates were explored that are potent inhibitors...
A series of phenyl piperidine α-sulfone hydroxamate derivatives has been prepared utilizing a combin...
A series of N-aryl isonipecotamide α-sulfone hydroxamate derivatives has been prepared utilizing a c...
A series of α-alkyl-α-amino-β-sulphone hydroxamates was prepared and evaluated for potency versus MM...
α-Piperidine-β-sulfone hydroxamate derivatives were explored that are potent for matrix metalloprote...
A series of α-amino-β-sulphone hydroxamates was prepared and evaluated for potency versus MMP-13 and...
Purpose: The implication of matrix metalloproteinases (MMPs) in the major stages of cancer progressi...
Matrix metalloproteinase 7 (MMP-7) is a member of the MMP superfamily and is able to degrade extrace...
Continuing our interest in designing compounds preferentially potent and selective for MMP-13, we re...
Collagen degradation and proMMP-2 activation are major functions of MT1-MMP to promote cancer cell i...
Gelatinase B or matrix metalloproteinase-9 (MMP-9) (EC 3.4.24.35) is increased in inflammatory proce...
Seeking compounds preferentially potent and selective for MMP-13, we reported in the preceding Lette...
We recently reported the discovery of AM-8553 (<b>1</b>), a potent and selective piperidinone inhibi...
Osteoarthritis (OA) is the leading cause of joint pain and disability in middle-aged and elderly pat...
Matrix metalloproteinases (MMPs) are a family of enzymes involved at different stages of cancer prog...