eng URI http://hdl.handle.net/10795/2598 βιοχημεία ένζυμο βιοτεχνολογία φαρμακευτικό προϊόν Over expression of human GSTA1-1 in tumour cells is part of MDR mechanisms. Substituted 2-hydroxybenzophenones are ubiquitous in naturally occurring and synthetic compounds, exhibiting important biological activities. 2,2’-Dihydroxybenzophenones and N-carbonyl analogues, structurally, are ringopened forms of xanthone analogues which we reported recently as hGSTA1-1 inhibitors. The present study combined GST inhibition screening, in silico molecular docking and enzyme inhibition kinetics, revealing four analogues with strong inhibitory potency (IC50 = 0.18-1.8 μM) and modest cytotoxic activity for Caco2 cell line (LC50 = 35 to > 400 μM), thus being useful as lead structures for the design of new inhibitors against hGSTs. 1 pp. LOMv1.0 creator LOMv1.0 Project Final Beneficiary LOMv1.0 Project Executing Organisation 2015 Digital Library of the Operational Programme "Education and Lifelong Learning" abstract types Text Glutathione S-transferase Inhibitors N-carbonyl analogues Biotechnology Biology Human GSTs Biochemistry 3123768 application/pdf http://repository.edulll.gr/edulll/bitstream/10795/2598/2/2598_Poster%204.pdf URI http://hdl.handle.net/10795/2598 LOMv1.0creator 2016-04-13T10:15:48Z LOMv1.0validator 2016-04-13T10:15:48Z LOMv1.0 gre no no Copyright EYD-EPEDBM (Operational Programme "Education and Lifelong Learning")