Synthesis and antileukemic activity of novel 2‐(4‐(2, 4‐dimethoxybenzoyl) phenoxy)‐1‐(4‐(3‐(piperidin‐4‐yl) propyl) piperidin‐1‐yl) ethanone derivatives

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 ¹H 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 IC₅₀values 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).