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).
|Autori:||A. ROSSELLO; E. NUTI; ORLANDINI E; P. CARELLI; S. RAPPOSELLI; M. MACCHIA; F. MINUTOLO; L. CARBONARO; A. ALBINI; R. BENELLI; G. CERCIGNANI; G. MURPHY; A. BALSAMO|
|Titolo:||New N-arylsulfonyl-N-alkoxyaminoacetohydroxamic acids as selective inhibitors of gelatinase A (MMP-2)|
|Anno del prodotto:||2004|
|Digital Object Identifier (DOI):||10.1016/j.bmc.2004.01.047|
|Appare nelle tipologie:||1.1 Articolo in rivista|