Journal
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
Volume 30, Issue 3, Pages 371-376Publisher
TAYLOR & FRANCIS LTD
DOI: 10.3109/14756366.2014.940932
Keywords
1,3-dipolar cycloaddition; anti-5-lipoxygenase; anti-acetylcholinesterase; anti-cancer; harmine; oxazolines; Peganum harmala
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In our study, a series of new harmine derivatives has been prepared by cycloaddition reaction using various arylnitrile oxides and evaluated in vitro against acetylcholinesterase and 5-lipoxygenase enzymes, MCF7 and HCT116 cancer cell lines. Some of these molecules have been shown to be potent inhibitors of acetylcholinesterase and MCF7 cell line. The greatest activity against acetylcholinesterase (IC50 = 10.4 mu M) was obtained for harmine 1 and cytotoxic activities (IC50 = 0.2 mu M) for compound 3a. Two derivatives 3e and 3f with the thiophene and furan systems, respectively, showed good activity against 5-lipoxygenase enzyme (IC50 - 29.2 and 55.5 mu M, respectively).
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