Paper
Novel N-(2-Methoxydibenzofuran-3-yl)-2-aryloxyacetamide Derivatives: Synthesis and Biological Investigation
Published Nov 10, 2020 · Leyla Yurttaş, B. Çavușoğlu, H. Temel
Letters in Drug Design & Discovery
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Abstract
Dibenzofuran ring is a typical heterocyle that is found in many natural sources and its derivatives exhibit a wide scale of biological applications similar to its analog ring systems; furan and benzofuran. Novel N-(2-methoxydibenzofuran-3-yl)-2-aryloxyacetamide derivatives (2a-l) were synthesized and evaluated for their cytotoxic activity against A549 lung cancer and NIH/3T3 mouse embryofibroblast cell lines. The inhibition percentages of cathepsin D, L, acetylcholinesterase (AChE) and butrylcholinesterase (BuChE) enzymes provoked by the compounds were also determined. Most of the compounds exhibited significant cytotoxicity whose IC50 values were identified lower than the tested lowest concentration (<3.90 μg/mL). Compound 2i against cathepsin D and compound 2k against cathepsin L displayed the highest inhibitory activity. Regrettably, the compounds demonstrated very weak AChE and BuChE inhibition. Compounds 2b, 2c, 2e, 2i and 2k exhibited the highest antiproliferative activity against A549 cell lines with selective profile. However, they did not display satisfying results on tested enzymes.
Novel N-(2-methoxydibenzofuran-3-yl)-2-aryloxyacetamide derivatives show significant cytotoxicity against A549 lung cancer and NIH/3T3 mouse embryofibroblast cells, with compounds 2i and 2k showing the highest inhibitory activity against cathep
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