Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10598793 | Bioorganic & Medicinal Chemistry Letters | 2005 | 6 Pages |
Abstract
Structural manipulation of the pharmacophoric model of type A selective MMP inhibitors (MMPi), obtained by the insertion of some alkyl substituents R2 possessing an appropriate geometry, steric bulkiness and lipophilicity, is able to improve potency, in the subnanomolar range on MMP-2, and to give a good MMP inhibition on MMP-14 (MT1-MMP) in the designed MMPi of type C, while maintaining a good MMP-1/MMP-2 selectivity profile. The simultaneous inhibition of these two enzymes yields type C compounds, which are potent antiangiogenic agents, able to block a chemoinvasion model on HUVEC cells under the micromolar range.
Keywords
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Armando Rossello, Elisa Nuti, Paolo Carelli, Elisabetta Orlandini, Marco Macchia, Susanna Nencetti, Maurizio Zandomeneghi, Federica Balzano, Gloria Uccello Barretta, Adriana Albini, Roberto Benelli, Giovanni Cercignani, Gillian Murphy, Aldo Balsamo,