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Synthesis and antileukemic activity of novel 2-(4-(2,4-dimethoxybenzoyl)phenoxy)-1-(4-(3-(piperidin-4-yl)propyl)piperidin-1-yl)ethanone derivatives
Authors:Vinaya Kambappa  Kavitha Chandagirikoppal V  Prasanna Doddakunche S  Chandrappa Siddappa  Ranganatha Somasagara R  Raghavan Sathees C  Rangappa Kanchugarakoppal S
Institution:1. Department of Studies in Chemistry, University of Mysore, Manasagangotri, Mysore 570 006, India;2. Department of Chemistry, Government First Grade College, Kadur 577 548, India;3. Department of Biochemistry, Indian Institute of Science, Bangalore 560 012, India;4. Department of Chemistry, Government College for Women, Mandya 571 401, India;5. Post‐graduate Department of Studies in Chemistry, JSS College of Arts, Commerce and Science, Ooty Road, Mysore 570 025, India
Abstract:A series of novel 2-(4-(2,4-dimethoxybenzoyl)phenoxy)-1-(4-(3-(piperidin-4-yl)propyl) piperidin-1-yl)ethanone derivatives 9(a-e) and 10(a-g) were synthesized and characterized by (1) H NMR, IR, mass spectral, and elemental analysis. These novel compounds were evaluated for their antileukemic activity against two human leukemic cell lines (K562 and CEM) by using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazoliumbromide assay. Some of the tested compounds showed good antiproliferative activity with IC(50) values ranging from 1.6 to 8.0 μm. Compound 9c, 9e, and 10f with an electron-withdrawing halogen substituent at the para position on the phenyl ring showed excellent in vitro potency against tested human leukemia cells (K562 and CEM).
Keywords:1  3‐dimethoxy benzene  anticancer agents  cell death  leukemia  MTT assay  piperidine
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