Synthesis and Antileukemic Activity of Novel 2-(4-(2,4-dimethoxybenzoyl)phenoxy)-1-(4-(3-(piperidin-4-yl)propyl)piperidin-1-yl)ethanone Derivatives

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 a...

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Veröffentlicht in:Chemical biology & drug design 2012-03, Vol.79 (3), p.360-367
Hauptverfasser: Vinaya, Kambappa, Kavitha, Chandagirikoppal V., Prasanna, Doddakunche S., Chandrappa, Siddappa, Ranganatha, Somasagara R., Raghavan, Sathees C., Rangappa, Kanchugarakoppal S.
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Sprache:eng
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Zusammenfassung: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 IC50 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). A series of novel 2‐(4‐(2,4‐dimethoxybenzoyl)phenoxy)‐1‐(4‐(3‐(piperidin‐4‐yl)propyl) piperidin‐1‐yl)ethanone derivatives were synthesized and evaluated for their antileukemic activity against two human leukemic cell lines (K562 and CEM). Compound 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).
ISSN:1747-0277
1747-0285
DOI:10.1111/j.1747-0285.2011.01307.x