الفهرس 
INTRODUCTIONOnly 14 pages are availabe for public view
 |  | from | 161 |  |  |
| | | from | 161 | | |
Abstract
Twelve compounds were more active than the standard 5-FU against colon cancer cell lines (Caco-2 and HCT-116).
<Compounds 3aand 7awere the most potent (for Caco-2; IC50= 83.88 and 68.65μM, respectively vs 206.41 for 5-FUand for HCT-116; IC50= 65.71 and 47.59μM, respectively vs 179.28 for 5-FU).
< Interestingly, these data coincided with their PASS predictive values.
< Flow cytometric analysis of cell death for both compounds using annexin V/propidium iodide revealed that they induced apoptosis via caspase 3/7 activation in treated Caco-2 and HCT-116 cell lines.
In addition, they were more potent inhibitors of COX-2 and 15-LOX enzymes than celecoxib, zileuton and quercetin, respectively.
They showed significant anti-colitis activity with low EAIC values, being more potent than sulfasalazine.
They inhibited NO and TNF-α production in DSS-stimulated rat colonic leukocytes.
Compound 3aelicited higher antioxidant activity than the reference in DPPH and hydroxylradical assays while 7a showed its potency in DPPH, superoxide anion and ferrous reducing power assays.
Docking experiments on COX-2 and 15-LOX enzymes underlined favorable binding patterns.
Moreover, physicochemical properties, drug-likeness and ADMET parameters were also assessed.