title: Rapid assembly of matrix metalloprotease inhibitors using click chemistry.
abstract: [reaction: see text] A panel of 96 metalloprotease inhibitors was assembled using "click chemistry" by reacting eight zinc-binding hydroxamate warheads with 12 azide building blocks. Screens of the bidentate compounds against representative metalloproteases provided discerning inhibition fingerprints, revealing compounds with low micromolar potency against MMP-7. The relative ease and convenience of the strategy in constructing focused chemical libraries for rapid in situ screening of MMPs is thereby demonstrated.
authors.affiliation: Department of Chemistry, Medicinal Chemistry Program of the Office of Life Sciences, National University of Singapore, 3 Science Drive 3, Singapore 117543, Republic of Singapore.
authors.forename: Jun
authors.initials: J
authors.lastname: Wang
authors.forename: Mahesh
authors.initials: M
authors.lastname: Uttamchandani
authors.forename: Junqi
authors.initials: J
authors.lastname: Li
authors.forename: Mingyu
authors.initials: M
authors.lastname: Hu
authors.forename: Shao Q
authors.initials: SQ
authors.lastname: Yao
mesh_terms: D001407:Bacillus / Q000378:metabolism; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D006877:Hydroxamic Acids / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D061965:Matrix Metalloproteinase Inhibitors; D015394:Molecular Structure
chemical_list: D004791:Enzyme Inhibitors; D006877:Hydroxamic Acids; D061965:Matrix Metalloproteinase Inhibitors