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ID: ALA1130917

Journal: Bioorg Med Chem Lett

Title: The design, synthesis, and structure-activity relationships of a series of macrocyclic MMP inhibitors.

Authors: Steinman DH, Curtin ML, Garland RB, Davidsen SK, Heyman HR, Holms JH, Albert DH, Magoc TJ, Nagy IB, Marcotte PA, Li J, Morgan DW, Hutchins C, Summers JB.

Abstract: A series of succinate-derived hydroxamic acids incorporating a macrocyclic ring were designed, synthesized, and evaluated as inhibitors of matrix metalloproteinases. The inhibitors were designed based on the published X-ray crystal structure of batimastat (1) complexed with human neutrophil collagenase (MMP-8). The synthesized compounds were shown to inhibit selected MMPs in vitro with low nanomolar potency.

CiteXplore: 9873491

DOI: 10.1016/s0960-894x(98)00396-5