Author/Authors :
Armando Rossello، نويسنده , , Elisa Nuti، نويسنده , , Elisabetta Orlandini، نويسنده , , Paolo Carelli، نويسنده , , Simona Rapposelli، نويسنده , , Marco Macchia، نويسنده , , Filippo Minutolo، نويسنده , , Laura Carbonaro، نويسنده , , Adriana Albini، نويسنده , , Roberto Benelli، نويسنده , , Giovanni Cercignani، نويسنده , , Gillian Murphy، نويسنده , , Aldo Balsamo، نويسنده ,
Abstract :
New N-arylsulfonyl-substituted alkoxyaminoaceto hydroxamic acid derivatives of types 8 and 10 designed as oxa-analogues of known sulfonamide-based MMPi of types 2 and 7 were synthesized and tested for their inhibitory activities on some matrix metalloproteinases. The combination of a biphenylsulfonamide group with oxyamino oxygen in the pharmacophoric central skeleton of sulfonamide-based MMPi obtained in the new sulfonamides 10 seems to be able to give selectivity for MMP-2 over MMP-1. The most potent derivative of this type, 10a, shows similar anti-invasive properties to the analogue reference drug CGS27023A, 2, in an in vitro model of invasion on matrigel, carried out on cellular lines of fibrosarcoma HT1080 (tumoural cells over-expressing MMP-2 and MMP-9).
