Phosphinic acid inhibitors of matrix metalloproteinases

DOI: 10.1016/0960-894X(96)00023-6

Source and publish data:

Bioorganic and Medicinal Chemistry Letters p. 323 - 328 (1996)

Update date:2022-07-30

Topics:

Authors:

Caldwell

Sahoo Sahoo

Polo Polo

Eversole

Lanza Lanza

Mills Mills

Niedzwiecki

Izquierdo-Martin

Chang Chang

Harrison

Kuo Kuo

Lin Lin

Stein Stein

Durette Durette

Hagmann Hagmann

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Article abstract of DOI:10.1016/0960-894X(96)00023-6

The matrix metalloproteinase stromelyin-1 (MMP-3) is inhibited more strongly by peptidyl phosphinic acid 7 than by its corresponding phosphonamidate and phosphonate analogs. Extending a benzyl group at P₁' to a phenylethyl group in 8 further increases the potency (K(i) = 1.4 nM). Enhanced potency with an extended substituent into the P₃ region was observed.

Full text of DOI:10.1016/0960-894X(96)00023-6

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