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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
Author(s) -
Vinaya Kambappa,
Kavitha Chandagirikoppal V.,
Prasanna Doddakunche S.,
Chandrappa Siddappa,
Ranganatha Somasagara R.,
Raghavan Sathees C.,
Rangappa Kanchugarakoppal S.
Publication year - 2012
Publication title -
chemical biology and drug design
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.59
H-Index - 77
eISSN - 1747-0285
pISSN - 1747-0277
DOI - 10.1111/j.1747-0285.2011.01307.x
Subject(s) - chemistry , substituent , stereochemistry , k562 cells , ring (chemistry) , in vitro , potency , proton nmr , halogen , biochemistry , organic chemistry , alkyl
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 μ m . 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).