الفهرس | Only 14 pages are availabe for public view |
Abstract In this work, novel bisarylidene derivatives of cyclohexanone IIa-c, cyclopentanone IIIa-c, methyl piperidone IVa-c, 1-(phenylsulfonyl)piperidin-4-one VIa-c and 1-tosylpiperidin-4-one VIIa-c or arylidene derivatives of p-chloro acetophenone VIIIa-c were designed and synthesized as mono carbonyl analogues of curcumin (MACs) based on previous SAR studies of curcumin and its cyclohexanone derivative cyclovalone. All the synthesized compounds possessed Mannich base moiety in their aromatic rings. The target compounds were evaluated for their antiproliferative activity at the National Cancer Institute, NCI, Developmental therapeutic Program (DTP), Maryland, USA against a panel of sixty cell lines. Compounds IIIa-c, VIb and VIIa-c were promoted to the five-dose assay where they showed promising cytotoxic activities especially against leukemia SR and colon HT29 cell lines. The compounds were further screened for their cytotoxicity against HT29 colon cancer cell line where they showed promising activities in submicromolar level especially the piperidone derivatives |